Synthesis and antitumor activity of 1-deoxybaccatin III analogs from 1-deoxybaccatin VI
Synthesis and antitumor activity of 1-deoxybaccatin III analogs from 1-deoxybaccatin VI
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DOI：
10.1007/s00706-013-0981-z
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发表时间：
2013-08
期刊：
影响因子：
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通讯作者：
Yuan-You Qiu;Haixia Lin;Yongmei Cui;J. Shao;Dan Jin
中科院分区：
文献类型：
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作者：
Yuan-You Qiu;Haixia Lin;Yongmei Cui;J. Shao;Dan Jin
摘要以1-脱氧浆果赤霉素VI为原料合成了几种新的1-脱氧浆果赤霉素III类似物，目的是在C-2和C-4位上具有修饰的酯基。评价了这些化合物的抗肿瘤活性。初步的构效关系分析表明，C4、C9和C10上取代基的电子性质是影响其对A549和MCF-7细胞毒活性的重要因素。本研究为开发新的1-脱氧哌嗪类似物提供了新的合成基础。
AbstractSeveral new 1-deoxybaccatin III analogs were conveniently synthesized from 1-deoxybaccatin VI with the aim of having modified ester groups at C-2 and C-4. The antitumor activity of these compounds was evaluated. The preliminary SAR analysis showed that the electronic properties of the terminal group in the substituent on C4, C9, and C10 constituted important factors to the cytotoxic activities against A 549 and MCF-7 cell lines. The present studies provide a new synthetic basis for development of new 1-deoxypaclitaxel analogs.Graphical Abstract.