Synthesis and cytotoxic effect of pregnenolone derivatives with one or two α,β-unsaturated carbonyls and an ester moiety at C-21 or C-3

被引：5
作者：
Chavez-Riveros, Alejandra [1 ]
Cruz Noriega, Abigail [2 ]
Ramirez Apan, Maria Teresa [1 ]
Miranda, Luis D. [1 ]
Bratoeff, Eugene [2 ]
机构：
[1] Univ Nacl Autonoma Mexico, Inst Quim, Ciudad Univ, Cd Mx 04510, Mexico
[2] Univ Nacl Autonoma Mexico, Dept Farm, Fac Quim, Cd Mx 04510, Mexico
来源：
STEROIDS | 2018年 / 131卷
关键词：
Synthesis; Pregnenolone derivatives; Cytotoxicity; SKLU-1; PROGESTERONE DERIVATIVES; IN-VITRO; STEROIDS; CANCER; AGENTS; VIVO;
D O I：
10.1016/j.steroids.2018.01.004
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Four series of pregnenolone derivatives having one or two alpha,beta-unsaturated carbonyls and an ester moiety at C-21 or C-3 were synthetized to compare their cytotoxicity effect. The final compounds were evaluated on three human cancer cell lines: PC-3 (prostate cancer), MCF-7 (breast cancer), SKLU-1 (lung cancer) and a noncancerous cell line HGF (human gingival fibroblast). Two steroids with a 4-fluorinated benzoic acid ester at C-21 were the most active against lung cancer cell line with IC50 of 13.1 +/- 1.2 and 12.8 +/- 0.5 mu M and showed a low percentage of cytotoxicity for noncancerous cells (27.63 +/- 2.3 and 18.39 +/- 1.2% in the screening at 50 mu M).
引用
收藏
页码：37 / 45
页数：9
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