Synthesis and in vitro antitumor evaluation of betulin acid ester derivatives as novel apoptosis inducers.
Synthesis and in vitro antitumor evaluation of betulin acid ester derivatives as novel apoptosis inducers.
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DOI：
10.1016/j.ejmech.2015.08.004
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发表时间：
2015-09
影响因子：
6.7
通讯作者：
Shengjie Yang;Mingchuan Liu;Hongmei Xiang;Qi Zhao;Wei Xue;Song Yang
中科院分区：
文献类型：
--
作者：
Shengjie Yang;Mingchuan Liu;Hongmei Xiang;Qi Zhao;Wei Xue;Song Yang
Nineteen betulin derivatives modified at the C-3 and C-28 positions were synthesized and assessed for antitumor activities against the MGC-803, PC3, Bcap-37, A375, and MCF-7 human cancer cell lines in vitro by MTT assay. Some derivatives (compounds3a–3dand5) displayed strong antitumor properties, with IC50values between 4 and 18 μM. Compound3c, containing piperidine group at C-28 position, had IC50values of 4.3, 4.5, 5.2, 7.5, and 5.2 μM on the five cancer cell lines, respectively. Subsequent fluorescence staining and flow cytometric analysis indicated that compound3cinduced apoptosis in MGC-803 cell line, with an apoptosis ratio of 31.11% after 36 h of treatment at 10 μM3c.
