Recent advances in combretastatin based derivatives and prodrugs as antimitotic agents,RSC Medicinal Chemistry

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Recent advances in combretastatin based derivatives and prodrugs as antimitotic agents
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2017-07-04 00:00:00 , DOI: 10.1039/c7md00227k
Zaki S. Seddigi _{1,

2,

3,

4,

5} , M. Shaheer Malik _{3,

4,

5,

6} , A Prasanth Saraswati _{7,

8,

9,

10} , Saleh A. Ahmed _{3,

4,

5,

11,

12} , Ahmed O. Babalghith _{3,

4,

5,

13} , Hawazen A. Lamfon _{3,

4,

5,

12,

14} , Ahmed Kamal _{7,

8,

9,

10}

Affiliation

The dynamic and crucial role of tubulin in different cellular functions rendered it a promising target in anticancer drug development. Combretastatin A-4 (CA-4), an inhibitor of tubulin polymerization isolated from natural sources, is a lead molecule with significant cytotoxicity against tumour cells. Owing to its non polar nature it exhibits low solubility in natural biological fluids, thereby prompting the development of new CA-4 based derivatives. The modification of this lead molecule was mostly carried out by keeping the crucial cis-orientation of the double bond intact, along with a trimethoxyphenyl aromatic ring, by employing different approaches. The issue of solubility was also addressed by the development of water soluble prodrugs of CA-4. The present review highlights the investigations into the parallel development of both new CA-4 based derivatives and prodrugs in the past few years.

中文翻译：

基于康维他汀的衍生物和前药作为抗有丝分裂剂的最新进展

微管蛋白在不同细胞功能中的动态和关键作用使其成为抗癌药物开发的有希望的目标。Combretastatin A-4（CA-4）是从天然来源分离出的微管蛋白聚合抑制剂，是对肿瘤细胞具有明显细胞毒性的先导分子。由于其非极性性质，它在天然生物流体中显示出低溶解度，从而促进了新的基于CA-4的衍生物的开发。这种先导分子的修饰主要是通过保持关键的顺式进行的。通过采用不同的方法使完整的双键与三甲氧基苯基芳族环一起取向。通过开发CA-4的水溶性前药也解决了溶解性的问题。本综述重点介绍了过去几年对基于CA-4的新型衍生物和前药的并行开发研究。

更新日期：2017-08-16

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