Akhtar Md Jawaid, Yar M Shahar, Khan Ahsan Ahmed, Ali Zulphikar, Haider Md Rafi
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hamdard University, Hamdard Nagar, New Delhi- 110062, India.
Mini Rev Med Chem. 2017;17(17):1602-1632. doi: 10.2174/1389557516666161031121639.
The present review article presented a detailed account of the design strategies and the structure activity relationship of different derivatives apart from the nitrogen containing ring. These scaffolds play an important part in the drug discovery which showed anticancer activity against different human cancer cell lines through apoptosis, cell cycle arrest, inhibiting kinases, angiogenesis, disruption of cell migration, modulation of nuclear receptor responsiveness and others. Naphthalenes amides/amidines, furan, podophyllotoxin, platinum compounds, steroids, and urea, which forms the core part or along with other N-heterocyclic rings are enclosed. Some of these compounds e.g. podophyllotoxin and platinum based drugs displayed anticancer activity at nanomolar range. Various substitutions from the earlier and latest information are prerequisite in the drug synthesis process.
The review focused on the recent development of these derivatives, design and anticancer properties, thus providing with the most profound knowledge for the development of targeted based anticancer drugs.
本综述文章详细阐述了除含氮环之外的不同衍生物的设计策略及其构效关系。这些支架在药物研发中发挥着重要作用,通过诱导凋亡、使细胞周期停滞、抑制激酶、抑制血管生成、破坏细胞迁移、调节核受体反应性等方式,对不同的人类癌细胞系显示出抗癌活性。文中涵盖了萘酰胺/脒、呋喃、鬼臼毒素、铂化合物、甾体以及尿素,它们构成核心部分或与其他氮杂环一起。其中一些化合物,如鬼臼毒素和铂类药物,在纳摩尔浓度范围内显示出抗癌活性。在药物合成过程中,结合早期和最新信息进行各种取代是必不可少的。
本综述聚焦于这些衍生物的最新进展、设计及抗癌特性,从而为基于靶点的抗癌药物研发提供了最为深入的知识。