一些新型甾体 C-17 吡唑啉基衍生物的合成及细胞毒性活性。
Synthesis and cytotoxic activity of some novel steroidal C-17 pyrazolinyl derivatives.
机构信息
Shaanxi Engineering Center of Bioresource Chemistry & Sustainable Utilization, College of Science, Northwest A&F University, Yangling, Shaanxi 712100, China.
出版信息
Eur J Med Chem. 2013 Nov;69:182-90. doi: 10.1016/j.ejmech.2013.08.016. Epub 2013 Aug 19.
Fourteen novel steroidal C-17 pyrazolinyl derivatives 9a-g and 10a-g were synthesized from commercially available progesterone and tested for their cytotoxic activity against brine shrimp (Artemia salina) and three human cancer cell lines (NCI-H460, HeLa, and HepG2). Some of these synthetic compounds exhibited significant cytotoxic activity, and treatment of HeLa cells with compound 10b resulted in the cell population arrest in the S phase. A structure-activity relationship was discussed.
合成了 14 种新型甾体 C-17 吡唑啉基衍生物 9a-g 和 10a-g，从商业可得的黄体酮出发，对其进行了卤虫（盐水虾）和三种人类癌细胞系（NCI-H460、Hela 和 HepG2）的细胞毒性活性测试。其中一些合成化合物表现出显著的细胞毒性活性，用化合物 10b 处理 Hela 细胞导致细胞群体停滞在 S 期。讨论了构效关系。
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