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.

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.

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.

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.

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.

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.