Synthetic routes and biological evaluation of largazole and its analogues as potent histone deacetylase inhibitors.
Synthetic routes and biological evaluation of largazole and its analogues as potent histone deacetylase inhibitors.
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拉格唑及其类似物作为有效组蛋白脱乙酰酶抑制剂的合成路线和生物学评价
DOI：
10.3390/molecules16064681
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发表时间：
2011-06-07
期刊：
影响因子：
--
通讯作者：
Jiang S
中科院分区：
文献类型：
--
作者：
Li S;Yao H;Xu J;Jiang S
具有有趣的生物学特性和结构多样性的天然产物通常作为治疗各种人类疾病的有价值的先导候选药物。从海洋蓝细菌Symploca sp.中分离出的Largazole对许多癌细胞系表现出有效的抑制活性。此外，它在转化细胞和非转化细胞之间显示出显著的选择性，这是其他抗肿瘤天然产物如紫杉醇和放线菌素D的主要缺点。由于其作为一种有效的和选择性的抗癌药物候选人的潜力，大量的注意力已经集中在largazole及其类似物。本文综述了largazole及其类似物的合成及其构效关系的初步研究。
Natural products with interesting biological properties and structural diversity have often served as valuable lead drug candidates for the treatment of various human diseases. Largazole, isolated from the marine cyanobacterium Symploca sp. has exhibited potent inhibitory activity against many cancer cell lines. Besides, it shows remarkable selectivity between transformed and nontransformed cells, which is the main disadvantage of other antitumor natural products such as paclitaxel and actinomycin D. Due to its potential as a potent and selective anticancer drug candidate, a great deal of attention has been focused on largazole and its analogues. It is the aim of this review to highlight synthetic aspects of largazole and its analogues as well as their preliminary structure–activity relationship studies.
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