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Synthetic Routes and Biological Evaluation of Largazole and Its Analogues as Potent Histone Deacetylase Inhibitors

机译:拉加唑及其类似物作为有效组蛋白脱乙酰基酶抑制剂的合成途径和生物学评价

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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.
机译:具有令人感兴趣的生物学特性和结构多样性的天然产物通常用作治疗各种人类疾病的有价值的先导药物。拉加唑,从海洋蓝藻Symploca sp。分离。已经显示出对许多癌细胞系的有效抑制活性。此外,它在转化细胞和未转化细胞之间显示出显着的选择性,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。由于其作为有效的选择性抗癌药物的潜力,因此引起了广泛关注largazole及其类似物上。这篇综述的目的是突出拉拉唑及其类似物的合成方面,以及它们的初步结构-活性关系研究。

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    《Molecules》 |2011年第6期|共14页
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  • 中图分类 有机化学;
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