Design And Synthesis Of Organic Molecules As Antineoplastic Agents

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Design and Synthesis of Organic Molecules as Antineoplastic Agents

Author : Carla Boga
Publisher : MDPI
ISBN 13 : 3039366661
Total Pages : 210 pages
Book Rating : 4.0/5 (393 download)

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Book Synopsis Design and Synthesis of Organic Molecules as Antineoplastic Agents by : Carla Boga

Download or read book Design and Synthesis of Organic Molecules as Antineoplastic Agents written by Carla Boga and published by MDPI. This book was released on 2020-12-28 with total page 210 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book is a collection of Special Issue articles with a multidisciplinary character, linking biology, medicine, and synthetic organic chemistry. The synthesis and full characterization of about 180 novel organic species, both of natural and synthetic origin, often designed with the support of in-silico studies, are set out in the book. In several articles, molecular hybridization approaches have been used as a successful multi-target strategy for the design and development of novel antitumor agents. Rigorous and careful biochemical studies ranging from in-vitro experiments on a plethora of human-cancer derived cell lines to in-vivo and ex-vivo studies allowed the authors to identify the molecular targets and gain useful information on structure–activity relationships (SAR). For this reason, this collection should interest many readers from different scientific fields.

Design and Synthesis of Organic Molecules as Antineoplastic Agents

Author : Carla Boga
Publisher :
ISBN 13 : 9783039366675
Total Pages : 210 pages
Book Rating : 4.3/5 (666 download)

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Book Synopsis Design and Synthesis of Organic Molecules as Antineoplastic Agents by : Carla Boga

Download or read book Design and Synthesis of Organic Molecules as Antineoplastic Agents written by Carla Boga and published by . This book was released on 2020 with total page 210 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book is a collection of Special Issue articles with a multidisciplinary character, linking biology, medicine, and synthetic organic chemistry. The synthesis and full characterization of about 180 novel organic species, both of natural and synthetic origin, often designed with the support of in-silico studies, are set out in the book. In several articles, molecular hybridization approaches have been used as a successful multi-target strategy for the design and development of novel antitumor agents. Rigorous and careful biochemical studies ranging from in-vitro experiments on a plethora of human-cancer derived cell lines to in-vivo and ex-vivo studies allowed the authors to identify the molecular targets and gain useful information on structure-activity relationships (SAR). For this reason, this collection should interest many readers from different scientific fields.

Anticancer Agents

Author : Qiao-Hong Chen
Publisher : MDPI
ISBN 13 : 3036501401
Total Pages : 606 pages
Book Rating : 4.0/5 (365 download)

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Book Synopsis Anticancer Agents by : Qiao-Hong Chen

Download or read book Anticancer Agents written by Qiao-Hong Chen and published by MDPI. This book was released on 2021-03-02 with total page 606 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book is a printed edition of the Special Issue entitled “Anticancer Agents: Design, Synthesis and Evaluation” that was published in Molecules. Two review articles and thirty research papers are included in the Special Issue. Three second-generation androgen receptor antagonists that have been approved by the U.S. FDA for the treatment of prostate cancer have been reviewed. Identification of mimics of protein partners as protein-protein interaction inhibitors via virtual screening has been summarized and discussed. Anticancer agents targeting various protein targets, including IGF-1R, Src, protein kinase, aromatase, HDAC, PARP, Toll-Like receptor, c-Met, PI3Kdelta, topoisomerase II, p53, and indoleamine 2,3-dioxygenase, have been explored. The analogs of three well-known tubulin-interacting natural products, paclitaxel, zampanolide, and colchicine, have been designed, synthesized, and evaluated. Several anticancer agents representing diverse chemical scaffolds were assessed in different kinds of cancer cell models. The capability of some anticancer agents to overcome the resistance to currently available drugs was also studied. In addition to looking into the in vitro ability of the anticancer agents to inhibit cancer cell proliferation, apoptosis, and cell cycle, in vivo antitumor efficacy in animal models and DFT were also investigated in some papers.

Anticancer Agents

Author : Qiao-Hong Chen
Publisher :
ISBN 13 : 9783036501413
Total Pages : 606 pages
Book Rating : 4.5/5 (14 download)

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Book Synopsis Anticancer Agents by : Qiao-Hong Chen

Download or read book Anticancer Agents written by Qiao-Hong Chen and published by . This book was released on 2021 with total page 606 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book is a printed edition of the Special Issue entitled “Anticancer Agents: Design, Synthesis and Evaluation” that was published in Molecules. Two review articles and thirty research papers are included in the Special Issue. Three second-generation androgen receptor antagonists that have been approved by the U.S. FDA for the treatment of prostate cancer have been reviewed. Identification of mimics of protein partners as protein-protein interaction inhibitors via virtual screening has been summarized and discussed. Anticancer agents targeting various protein targets, including IGF-1R, Src, protein kinase, aromatase, HDAC, PARP, Toll-Like receptor, c-Met, PI3Kdelta, topoisomerase II, p53, and indoleamine 2,3-dioxygenase, have been explored. The analogs of three well-known tubulin-interacting natural products, paclitaxel, zampanolide, and colchicine, have been designed, synthesized, and evaluated. Several anticancer agents representing diverse chemical scaffolds were assessed in different kinds of cancer cell models. The capability of some anticancer agents to overcome the resistance to currently available drugs was also studied. In addition to looking into the in vitro ability of the anticancer agents to inhibit cancer cell proliferation, apoptosis, and cell cycle, in vivo antitumor efficacy in animal models and DFT were also investigated in some papers.

Antineoplastic Drugs

Author : Daniel Lednicer
Publisher : John Wiley & Sons
ISBN 13 : 1118892569
Total Pages : 227 pages
Book Rating : 4.1/5 (188 download)

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Book Synopsis Antineoplastic Drugs by : Daniel Lednicer

Download or read book Antineoplastic Drugs written by Daniel Lednicer and published by John Wiley & Sons. This book was released on 2015-03-11 with total page 227 pages. Available in PDF, EPUB and Kindle. Book excerpt: The past decade has seen a significant increase of research aimed at discovering new drugs for treating cancer, and the increasing number of new antineoplastic drugs approved by regulatory agencies reflects this. Until now, details on the synthesis of these newer agents have been scattered in various journals and in US and European patents. This timely volume deals with the organic chemistry involved in the synthesis of the agents found within antineoplastic drugs, including descriptions of the synthetic schemes for the preparation of over 200 compounds that have been granted non-proprietary names. Compounds are collected in chapters based on the mechanism of action rather than on their chemical structures. Each individual chapter is preceded by a brief description of that mechanism and includes detailed flow charts of the preparation of those compounds accompanied by discussions of the organic chemistry involved in each step. The first half of this volume is dedicated to the syntheses of established chemotherapy drugs. Kinase inhibitors occupy the following chapters with the largest single chapter dealing with the fifty compounds that inhibit tyrosine kinase. This class stands out since over twenty compounds in this group have been approved for treating patients; a rare track record compared to any other class of therapeutic agents. Antineoplastic Drugs: Organic Syntheses is written to appeal to organic and medicinal chemists in industry and academia. It is beneficial to those composing grant proposals for NCI and related organizations. The book is accessible to advanced undergraduates as well as graduates and researchers as well as those with a thorough grasp of organic chemistry.

Design and Synthesis of Organic Molecules Based on Molecular Recognition

Author : Georges van Binst
Publisher : Springer
ISBN 13 :
Total Pages : 340 pages
Book Rating : 4.3/5 (91 download)

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Book Synopsis Design and Synthesis of Organic Molecules Based on Molecular Recognition by : Georges van Binst

Download or read book Design and Synthesis of Organic Molecules Based on Molecular Recognition written by Georges van Binst and published by Springer. This book was released on 1986 with total page 340 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Heterocyclic Anticancer Agents

Author : Bimal Krishna Banik
Publisher : Walter de Gruyter GmbH & Co KG
ISBN 13 : 3110735776
Total Pages : 532 pages
Book Rating : 4.1/5 (17 download)

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Book Synopsis Heterocyclic Anticancer Agents by : Bimal Krishna Banik

Download or read book Heterocyclic Anticancer Agents written by Bimal Krishna Banik and published by Walter de Gruyter GmbH & Co KG. This book was released on 2022-06-21 with total page 532 pages. Available in PDF, EPUB and Kindle. Book excerpt: Cancer is an incredibly diverse and difficult disease to treat, and even after decades of research there is no definitive cure. Therefore, it is highly crucial to search for novel and new organic molecules with high potency, low toxicity, and low mutagenicity with selective anticancer properties that are able to overcome frequently developed resistance to available drugs. Heterocyclic anticancer agents are an important class of drugs for cancer therapies. This book explores different heterocycles and their use as anticancer therapies. Topics covered include different heterocyclic derivatives, the impact of heterocycles on anticancer agent development, and naturally occurring heterocycles.

Exercises in Organic Synthesis Based on Synthetic Drugs

Author : Marcus Vinícius Nora de Souza
Publisher : Bentham Science Publishers
ISBN 13 : 9811487545
Total Pages : 250 pages
Book Rating : 4.8/5 (114 download)

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Book Synopsis Exercises in Organic Synthesis Based on Synthetic Drugs by : Marcus Vinícius Nora de Souza

Download or read book Exercises in Organic Synthesis Based on Synthetic Drugs written by Marcus Vinícius Nora de Souza and published by Bentham Science Publishers. This book was released on 2020-12-23 with total page 250 pages. Available in PDF, EPUB and Kindle. Book excerpt: Exercises in Organic Synthesis Based on Synthetic Drugs presents information on topics about the synthesis of biologically active compounds which are used against a range of diseases in both humans and animals. Topics are supplemented by notes and exercises for students to stimulate inquiry and learning in the academic environment. Readers will be equipped with basic knowledge of synthetic techniques used in organic chemistry and pharmaceutical research and development. Key Features: - Presents information about different techniques and strategies for the synthesis of organic compounds - Covers a broad range of biologically active compounds - Easy to read topical presentation - Exercises, with answers, designed for improving concepts in organic synthesis and medicinal chemistry - Wide range of bibliographic references for further reading and exercises presented, Exercises in Organic Synthesis Based on Synthetic Drugs is an essential textbook for students in beginner level courses in organic chemistry, organic synthesis and medicinal chemistry.

Design and Synthesis of Novel Compounds as Therapeutic Agents

Author : Mariam S. Shafqat
Publisher :
ISBN 13 :
Total Pages : 0 pages
Book Rating : 4.:/5 (14 download)

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Book Synopsis Design and Synthesis of Novel Compounds as Therapeutic Agents by : Mariam S. Shafqat

Download or read book Design and Synthesis of Novel Compounds as Therapeutic Agents written by Mariam S. Shafqat and published by . This book was released on 2023 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: Novel chemical moieties have been developed using structure-based drug design for the treatment of type 1 diabetes mellitus and cancer. In my first project, I studied novel small molecules for type 1 diabetes. Diabetes is an incurable, lifetime disease affecting millions of people worldwide. Our collaborators identified that the commercially available hydrazone moiety, EPB-1, increases insulin secretion while simultaneously protecting against pancreatic cell death making it a dual-function drug specifically targeted for type 1 diabetes. This compound’s unique dual-functional bioactivity has led us to explore hydrazones and other small molecules to uncover a new lead compound via structure-based drug design. A total of three generations of compounds have been synthesized and evaluated to identify the indazole-based amide, MSB-61, as a more potent analog making it our current lead compound. My second project investigates natural product-based analogs as potential anticancer agents. Natural products are an underexplored class of compounds with hidden potential. The commercially available, cheap raw material Stevioside is subjected to acid hydrolysis to isolate the natural product isosteviol. The skeletally diverse and stereochemically complex isosteviol scaffold has been used as the backbone to design analogs that exhibit a broad range of bioactivity including antimicrobial, antituberculosis, and cardioprotective properties. This research focuses on utilizing organic. synthetic techniques, such as the multicomponent Ugi reaction, to design and generate a compound library of isosteviol-based analogs as anticancer agents.

Green Chemistry

Author : Hosam El-Din M. Saleh
Publisher : BoD – Books on Demand
ISBN 13 : 9535138472
Total Pages : 191 pages
Book Rating : 4.5/5 (351 download)

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Book Synopsis Green Chemistry by : Hosam El-Din M. Saleh

Download or read book Green Chemistry written by Hosam El-Din M. Saleh and published by BoD – Books on Demand. This book was released on 2018-02-28 with total page 191 pages. Available in PDF, EPUB and Kindle. Book excerpt: To an increasing extent, "green chemistry" is a new chemical and engineering approach of chemistry and engineering, dedicated to make manufacturing processes and our world as a whole more sustainable world with a growing tendency. "Green chemistry" approaches are based on ecofriendly technologies, aiming to reduce or eliminate the use of solvents, or render them efficient and safer. Moreover, this scientific field is devoted to reduction or elimination of prevailing environmental and health threats, which typically accompany chemical products and traditional processes. The present book "Green Chemistry" contains 9 selected chapters, starting with a general introductory chapter on "green chemistry," and covers many recent applications and developments based on the principles of "green chemistry." This book is considered the appropriate way to communicate the advances in green materials and their applications to the scientific community. Chemists, scientists and researchers from related areas, and undergraduates involved in environmental issues and interested in approaches to improve the quality of life could find an inspiring and effective guide by reading this book.

Drug-like Properties: Concepts, Structure Design and Methods

Author : Li Di
Publisher : Elsevier
ISBN 13 : 0080557619
Total Pages : 549 pages
Book Rating : 4.0/5 (85 download)

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Book Synopsis Drug-like Properties: Concepts, Structure Design and Methods by : Li Di

Download or read book Drug-like Properties: Concepts, Structure Design and Methods written by Li Di and published by Elsevier. This book was released on 2010-07-26 with total page 549 pages. Available in PDF, EPUB and Kindle. Book excerpt: Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, typically only a fraction of these have sufficient ADME/Tox properties to become a drug product. Understanding ADME/Tox is critical for all drug researchers, owing to its increasing importance in advancing high quality candidates to clinical studies and the processes of drug discovery. If the properties are weak, the candidate will have a high risk of failure or be less desirable as a drug product. This book is a tool and resource for scientists engaged in, or preparing for, the selection and optimization process. The authors describe how properties affect in vivo pharmacological activity and impact in vitro assays. Individual drug-like properties are discussed from a practical point of view, such as solubility, permeability and metabolic stability, with regard to fundamental understanding, applications of property data in drug discovery and examples of structural modifications that have achieved improved property performance. The authors also review various methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties. Serves as an essential working handbook aimed at scientists and students in medicinal chemistry Provides practical, step-by-step guidance on property fundamentals, effects, structure-property relationships, and structure modification strategies Discusses improvements in pharmacokinetics from a practical chemist's standpoint

Medicinal Chemistry of Anticancer Drugs

Author : Carmen Avendaño
Publisher : Elsevier
ISBN 13 : 0444626670
Total Pages : 767 pages
Book Rating : 4.4/5 (446 download)

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Book Synopsis Medicinal Chemistry of Anticancer Drugs by : Carmen Avendaño

Download or read book Medicinal Chemistry of Anticancer Drugs written by Carmen Avendaño and published by Elsevier. This book was released on 2015-06-11 with total page 767 pages. Available in PDF, EPUB and Kindle. Book excerpt: Medicinal Chemistry of Anticancer Drugs, Second Edition, provides an updated treatment from the point of view of medicinal chemistry and drug design, focusing on the mechanism of action of antitumor drugs from the molecular level, and on the relationship between chemical structure and chemical and biochemical reactivity of antitumor agents. Antitumor chemotherapy is a very active field of research, and a huge amount of information on the topic is generated every year. Cytotoxic chemotherapy is gradually being supplemented by a new generation of drugs that recognize specific targets on the surface or inside cancer cells, and resistance to antitumor drugs continues to be investigated. While these therapies are in their infancy, they hold promise of more effective therapies with fewer side effects. Although many books are available that deal with clinical aspects of cancer chemotherapy, this book provides a sorely needed update from the point of view of medicinal chemistry and drug design. Presents information in a clear and concise way using a large number of figures Historical background provides insights on how the process of drug discovery in the anticancer field has evolved Extensive references to primary literature

Structure-based Design of Drugs and Other Bioactive Molecules

Author : Arun K. Ghosh
Publisher : John Wiley & Sons
ISBN 13 : 3527333657
Total Pages : 474 pages
Book Rating : 4.5/5 (273 download)

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Book Synopsis Structure-based Design of Drugs and Other Bioactive Molecules by : Arun K. Ghosh

Download or read book Structure-based Design of Drugs and Other Bioactive Molecules written by Arun K. Ghosh and published by John Wiley & Sons. This book was released on 2014-08-11 with total page 474 pages. Available in PDF, EPUB and Kindle. Book excerpt: Drug design is a complex, challenging and innovative research area. Structure-based molecular design has transformed the drug discovery approach in modern medicine. Traditionally, focus has been placed on computational, structural or synthetic methods only in isolation. This one-of-akind guide integrates all three skill sets for a complete picture of contemporary structure-based design. This practical approach provides the tools to develop a high-affinity ligand with drug-like properties for a given drug target for which a high-resolution structure exists. The authors use numerous examples of recently developed drugs to present "best practice" methods in structurebased drug design with both newcomers and practicing researchers in mind. By way of a carefully balanced mix of theoretical background and case studies from medicinal chemistry applications, readers will quickly and efficiently master the basic skills of successful drug design. This book is aimed at new and active medicinal chemists, biochemists, pharmacologists, natural product chemists and those working in drug discovery in the pharmaceutical industry. It is highly recommended as a desk reference to guide students in medicinal and chemical sciences as well as to aid researchers engaged in drug design today.

Beyond the Molecular Frontier

Author : National Research Council
Publisher : National Academies Press
ISBN 13 : 0309168392
Total Pages : 238 pages
Book Rating : 4.3/5 (91 download)

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Book Synopsis Beyond the Molecular Frontier by : National Research Council

Download or read book Beyond the Molecular Frontier written by National Research Council and published by National Academies Press. This book was released on 2003-03-19 with total page 238 pages. Available in PDF, EPUB and Kindle. Book excerpt: Chemistry and chemical engineering have changed significantly in the last decade. They have broadened their scopeâ€"into biology, nanotechnology, materials science, computation, and advanced methods of process systems engineering and controlâ€"so much that the programs in most chemistry and chemical engineering departments now barely resemble the classical notion of chemistry. Beyond the Molecular Frontier brings together research, discovery, and invention across the entire spectrum of the chemical sciencesâ€"from fundamental, molecular-level chemistry to large-scale chemical processing technology. This reflects the way the field has evolved, the synergy at universities between research and education in chemistry and chemical engineering, and the way chemists and chemical engineers work together in industry. The astonishing developments in science and engineering during the 20th century have made it possible to dream of new goals that might previously have been considered unthinkable. This book identifies the key opportunities and challenges for the chemical sciences, from basic research to societal needs and from terrorism defense to environmental protection, and it looks at the ways in which chemists and chemical engineers can work together to contribute to an improved future.

Medicinal Organometallic Chemistry

Author : Gérard Jaouen
Publisher : Springer Science & Business Media
ISBN 13 : 3642131840
Total Pages : 305 pages
Book Rating : 4.6/5 (421 download)

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Book Synopsis Medicinal Organometallic Chemistry by : Gérard Jaouen

Download or read book Medicinal Organometallic Chemistry written by Gérard Jaouen and published by Springer Science & Business Media. This book was released on 2010-09-14 with total page 305 pages. Available in PDF, EPUB and Kindle. Book excerpt: Contents: Gérard Jaouen, Nils Metzler-Nolte : Introduction ; Stéphane GIBAUD and Gérard JAOUEN: Arsenic - based drugs: from Fowler’s solution to modern anticancer chemotherapy; Ana M. Pizarro, Abraha Habtemariam and Peter J. Sadler : Activation Mechanisms for Organometallic Anticancer Complexes; Angela Casini, Christian G. Hartinger, Alexey A. Nazarov, Paul J. Dyson : Organometallic antitumour agents with alternative modes of action; Elizabeth A. Hillard, Anne Vessières, Gerard Jaouen : Ferrocene functionalized endocrine modulators for the treatment of cancer; Megan Hogan and Matthias Tacke : Titanocenes – Cytotoxic and Anti-Angiogenic Chemotherapy Against Advanced Renal-Cell Cancer; Seann P. Mulcahy and Eric Meggers : Organometallics as Structural Scaffolds for Enzyme Inhibitor Design; Christophe Biot and Daniel Dive : Bioorganometallic Chemistry and Malaria; Nils Metzler-Nolte : Biomedical applications of organometal-peptide conjugates; Roger Alberto : Organometallic Radiopharmaceuticals; Brian E. Mann : Carbon Monoxide – an essential signaling molecule.

The Organic Chemistry of Drug Synthesis, Volume 7

Author : Daniel Lednicer
Publisher : John Wiley & Sons
ISBN 13 : 0470180668
Total Pages : 288 pages
Book Rating : 4.4/5 (71 download)

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Book Synopsis The Organic Chemistry of Drug Synthesis, Volume 7 by : Daniel Lednicer

Download or read book The Organic Chemistry of Drug Synthesis, Volume 7 written by Daniel Lednicer and published by John Wiley & Sons. This book was released on 2007-12-14 with total page 288 pages. Available in PDF, EPUB and Kindle. Book excerpt: The classic reference on the synthesis of medicinal agents -- now completely updated The seventh volume in the definitive series that provides a quick yet thorough overview of the synthetic routes used to access specific classesof therapeutic agents, this volume covers approximately 220 new non-proprietary drug entities introduced since the publication of Volume 6. Many of these compounds represent novel structural types firstidentified by sophisticated new cell-based assays. Specifically, a significant number of new antineoplastic and antiviral agents are covered. As in the previous volumes, materials are organized by chemical class and syntheses originate with available starting materials. Organized to make the information accessible, this resource covers disease state, rationale for method of drug therapy, and the biological activities of each compound and preparation. The Organic Chemistry of Drug Synthesis, Volume 7 is a hands-on reference for medicinal and organic chemists, and a great resource for graduate and advanced undergraduate students in organic and medicinal chemistry.

Cellular and Phenotypic Plasticity in Cancer

Author : Petranel Theresa Ferrao
Publisher : Frontiers Media SA
ISBN 13 : 2889196623
Total Pages : 79 pages
Book Rating : 4.8/5 (891 download)

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Book Synopsis Cellular and Phenotypic Plasticity in Cancer by : Petranel Theresa Ferrao

Download or read book Cellular and Phenotypic Plasticity in Cancer written by Petranel Theresa Ferrao and published by Frontiers Media SA. This book was released on 2015-09-17 with total page 79 pages. Available in PDF, EPUB and Kindle. Book excerpt: The process of Epithelial-Mesenchymal-Transition (EMT) is known to result in a phenotype change in cells from a proliferative state to a more invasive state. EMT has been reported to drive the metastatic spread of various cancers and has also been associated with drug resistance to cytotoxics and targeted therapeutics. Recently phenotype switching akin to EMT has been reported in non-epithelial cancers such as metastatic melanoma. This process involves changes in EMT-Transcription Factors (EMT-TFs), suggesting that phenotype-switching may be common to several tumour types. It remains unclear as to whether the presence of both Epilthelial-like and Mesenchymal-like cells are a pre-requisite for phenotype switching within a tumour, how this heterogeneity is regulated, and if alteration of cell phenotype is sufficient to mediate migratory changes, or whether drivers of cell migration result in an associated phenotype switch in cancer cells. Similarly it has yet to be clarified if cells in an altered phenotype can be refractory to drug therapy or whether mediators of drug resistance induce a concurrent phenotypic change. Little is known today about the underlying genetic, epigenetic and transient changes that accompany this phenotypic switch and about the role for the tumor micro-environment in influencing it. Hence this is currently an area of speculation and keen interest in the Oncology field with wide-ranging translational implications. In this Frontiers Research Topic, we discuss our current understanding of these concepts in various cancer types including breast cancer, colorectal cancer and metastatic melanoma. This topic covers how these processes of cellular and phenotypic plasticity are regulated and how they relate to cancer initiation, progression, dormancy, metastases and response to cytotoxics or targeted therapies.