4.2 Article

Synthesis and antiproliferative activity of 17-[1′,2′,3′]-selenadiazolylpregnenolone compounds

期刊

STEROIDS
卷 140, 期 -, 页码 151-158

出版社

ELSEVIER SCIENCE INC
DOI: 10.1016/j.steroids.2018.10.004

关键词

17-[1 ',2 ',3 ']-Selenadiazolylpregnenolone; Antiproliferative activity; [1 ',2 ',3 ']-Selenadiazole; Pregnenolone; Organoselenium compounds

资金

  1. 'National Natural Science Foundation of China', China [21462009, 21562007]
  2. Nanning Technology Development Project of China [20171125-5]
  3. Universities Key Laboratory Funds of Synthetic and Natural Functional Molecular Chemistry

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Using pregnenolone as a starting material, some 3-substituted 17-[1',2',3']-selenadiazolylpregnenolone derivatives were synthesized, and their structures were characterized by IR, NMR and HRMS. The in vitro antitumor activity of the compounds was assayed against PC-3, SKOV3, T47D, MCF-7 and HEK293T cell lines. The results show that some compounds display selective antiproliferative activity against PC-3 and SKOV3 cells lines and are almost inactive to normal kidney epithelial cells (HEK293T). The IC50 value are much better than that of abiraterone (positive control).

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