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

页码：37 / 45

页数：9

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