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.

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 presents an overview of the recent advancements for the synthesis of small- and medium-sized azaheterocycles, including pyrroles, indoles, pyrimidines, pyridines, pyrrolidines, imidazoles, pyrazoles, pyrazolines, lactams, and 1,2,3-triazoles, which are significant scaffolds for compounds with pharmaceutical uses. The book also discusses various properties and performance attributes of azaheterocycles including their bioactivity and synthetic strategies. Given the contents, the book will be a valuable reference for students, researchers, and professionals interested in organic synthesis and medicinal chemistry.

Current Molecular Targets of Heterocyclic Compounds for Cancer Therapy discusses recently developed treatments based on molecular targets which are genetically altered in cancer cells and are essential for tumor development and survival. Considerable research effort has been devoted to the development of targeted drugs that inhibit the action of pathogenic kinases, and clinical studies performed so far have validated the positive effects of kinase inhibitors for cancer treatment. Each chapter discusses a molecular target, such as ALK2, ATR, CK, Src-Abl, EGFR, Fyn-Blk-Lyn, IGFs, and PAK1. The book's chapters are written by experts who actively work on the targets to help readers fully understand how they can be used. This is a valuable resource for cancer researchers, oncologists, graduate students and members of the biomedical field who are interested in the potential of novel cancer therapies based on molecular targets. - Discusses recently discovered molecular targets for cancer therapy - Brings updated literature of heterocyclic compounds, an important construction motif for the development of new anticancer drugs - Encompasses comprehensive compilation of recently introduced anticancer drugs in the market and their health outcomes and pharmacoeconomics