Evaluation of biological activity of new hemiesters of 17-hydroxy-16,17-secoestra-1,3,5(10)-triene-16-nitrile

被引：15

作者：

Jovanovic-Santa, Suzana S. ^{[1
]}

Andric, Silvana ^{[2
]}

Andric, Nebojsa ^{[2
]}

Bogdanovic, Gordana ^{[3
]}

Petrovic, Julijana A. ^{[1
]}

机构：

[1] Univ Novi Sad, Dept Chem, Fac Sci, Novi Sad 21000, Serbia

[2] Univ Novi Sad, Dept Biol & Ecol, Fac Sci, Novi Sad 21000, Serbia

[3] Oncol Inst Vojvodina, Sremska Kamenica 21204, Serbia

来源：

MEDICINAL CHEMISTRY RESEARCH | 2011年 / 20卷 / 07期

关键词：

16,17-Secoestratriene derivatives; Synthesis; Hemiesters; Antiestrogens; Aromatase inhibitors; Cytotoxicity; BREAST-CANCER; ESTROGEN-RECEPTORS; AROMATASE INHIBITION; ANTIESTROGEN ACTION; DERIVATIVES; ESTRADIOL; CELLS; RAT; CARCINOGENESIS; MEMBRANE;

D O I：

10.1007/s00044-010-9442-y

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In uterotrophic assay newly synthesized compounds 2-5 showed a complete loss of estrogenic activity, whereas derivatives 2-4 exhibited slight, and compound 5 higher antiestrogenic effects. On the other hand, anti-aromatase assay showed that compounds 2, 3, and 4 possess inhibition potency, although lower than standard aromatase inhibitor aminoglutethimide. Cytotoxicity of compounds 2-5, estradiol and tamoxifen against several human tumor or healthy cell lines (MCF-7, MDA-MB-231, HT-29, and MRC-5) was evaluated after short-time treatment.

引用

页码：1102 / 1110

页数：9

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