期刊
CURRENT TOPICS IN MEDICINAL CHEMISTRY
卷 14, 期 2, 页码 239-252出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1568026613666131216105049
关键词
Alkaloids; natural products; drugs; lead compounds; cancer; anticancer drugs; cytotoxic activity; antitubercular activity; antimycobacterial activity; tuberculosis; smoking cessation
资金
- Center of Excellence on Environmental Health and Toxicology, Science & Technology Postgraduate Education and Research Development Office (PERDO), Ministry of Education
Alkaloid molecules can act, depending on a type of amine functionality present in alkalods, as either hydrogen-acceptor or hydrogen-donor for hydrogen bonding that is critically important for the interaction (binding) between targets (enzymes, proteins and receptors) and drugs (ligands). Because of this unique property, alkaloid scaffolds are therefore present in several drugs and lead compounds. This review highlights alkaloid scaffolds in drugs, particularly those recently approved in 2012; it also covers the scaffolds in leads and drug candidates which are in clinical trials and preclinical pipeline. The review focuses on three therapeutic areas including treatments of cancer, tuberculosis, and tobacco cessation. Alkaloid scaffolds in drugs and leads are inspired by those of naturally occurring alkaloids, and these scaffolds include pyridine, piperidine, quinoline, quinolinone, quinazoline, isoquinoline, indole, indolinone, isoindole, isoxazole, imidazole, indazole, thiazole, pyrazole, oxazolidinone, oxadiazole, and benzazepine. In addition to medicinal chemistry aspects, natural products possessing an individual alkaloid scaffold, as well as the mechanism of action of drugs and leads, are also discussed in this review.
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