Synthesis and Biological Evaluation of 16E-Arylidenosteroids as Cytotoxic and Anti-aromatase Agents

被引：19

作者：

Bansal, Ranju ^{[1
]}

Guleria, Sheetal ^{[1
]}

Thota, Sridhar ^{[1
]}

Hartmann, Rolf Wolfgang ^{[2
]}

Zimmer, Christina ^{[2
]}

机构：

[1] Panjab Univ, Univ Inst Pharmaceut Sci, Sector 14, Chandigarh 160014, India

[2] Univ Saarland, D-66041 Saarbrucken, Germany

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 2011年 / 59卷 / 03期

关键词：

aromatase inhibitory activity; 16E-arylidenosteroid; dehyroepiandrosterone; cytotoxic activity; cancer cell line; breast cancer; NATIONAL-CANCER-INSTITUTE; DRUG DISCOVERY; BREAST-CANCER; DERIVATIVES; AMINOGLUTETHIMIDE; AROMATIZATION; INHIBITION; POTENT;

D O I：

10.1248/cpb.59.327

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Taking into consideration the structural requirements for cytotoxicity and aromatase inhibition, several new 16E-arylidenosteroidal derivatives have been prepared and evaluated for their cytotoxic and aromatase inhibitory activity. The new steroidal analogues 3, 5-8 and 11 exhibited significant cytotoxic effects when screened against three cancer cell lines, MCF-7 (breast), NCl-H460 (lung) and SF-268 central nervous system (CNS) at 100 mu m and sensible cytotoxic effects subsequently in sixty cancer cell lines derived from nine cancers types (leukemia, lung, colon, CNS, melanoma, ovarian, renal, prostate and breast cancers). The imidazolyl substituted steroidal derivatives 5 and 7 exhibited strong inhibition of the aromatase enzyme with 16-[4-{3-(imidazol-1-yl)propoxy}-3-methoxybenzylidene]-5-androstene-3 beta,17 beta-diol (7) displaying 13 times more potency in comparison to aminoglutethimide.

引用

页码：327 / 331

页数：5

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