Palladium-Catalyzed Synthesis and Anticancer Activity of Paclitaxel-Dehydroepiandrosterone Hybrids

被引：8
|
作者：
Lou, Sheng-Jie [2 ]
Li, Xiao-Huan [2 ]
Zhou, Xian-Li [2 ]
Fang, Dong-Mei [1 ]
Gao, Feng [2 ]
机构：
[1] Chinese Acad Sci, Chengdu Inst Biol, Chengdu 610041, Peoples R China
[2] Southwest Jiaotong Univ, Sch Life Sci & Engn, Chengdu 610031, Peoples R China
来源：
ACS OMEGA | 2020年 / 5卷 / 10期
关键词：
MICROTUBULE ASSEMBLY INVITRO; TAXOL; DESIGN; DERIVATIVES; GENERATION; CHEMISTRY; AGENTS; TOXICITY; PROSTATE; MIMICS;
D O I：
10.1021/acsomega.0c00558
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
According to the activity-structure relationship of the C-13 side chain in paclitaxel or docetaxel, eighteen novel paclitaxel-dehydroepiandrosterone (DHEA) hybrids were designed and synthesized by Pd(II)-catalyzed Suzuki-Miyaura cross-coupling of 17-trifluoromethanesulfonic enolate-DHEA with different aryl boronic acids. The in vitro anticancer activity of the hybrids against a human liver cancer cell line (HepG-2) was evaluated by MTT assay, showing that most of these hybrids possessed moderate antiproliferative activity against the HepG-2 cancer cell line. Among these hybrids, three ones (7b, 7g, and 7i) with ortho-substituents in the phenyl group of the D-ring of DHEA analogues exhibited moderate anticancer activity. The optimal compound 7i showed superior anticancer activity against the HepG-2 cell line with an IC50 value of 26.39 mu M.
引用
收藏
页码：5589 / 5600
页数：12
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