Synthesis, antiproliferative, acute toxicity and assessment of antiandrogenic activities of some newly synthesized steroidal lactams

被引：20
作者：
Dhingra, Neelima [1 ]
Bhardwaj, T. R. [1 ,3 ]
Mehta, Neeraj [1 ]
Mukhopadhyay, Tapas [2 ]
Kumar, Ashok [2 ]
Kumar, Manoj [1 ]
机构：
[1] Panjab Univ, Univ Inst Pharmaceut Sci, Chandigarh 160014, India
[2] Panjab Univ, Natl Ctr Human Genome Studies & Res, Chandigarh 160014, India
[3] ISF Coll Pharm, Moga 142001, India
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 06期
关键词：
Dihydrotestosterone; Five alpha reductase enzyme; Benign prostatic hyperplasia; 17a-Aza steroids; Androgen; BENIGN PROSTATIC HYPERPLASIA; REDUCED SYSTEMIC TOXICITY; 5-ALPHA-REDUCTASE INHIBITORS; CANCER CELLS; TESTOSTERONE; 4-AZASTEROIDS; APOPTOSIS; DESIGN; GROWTH; ENZYME;
D O I：
10.1016/j.ejmech.2010.01.064
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The 17-oxo-17a-aza-D-homo-5-androsten-3 beta-yl esters (13-22) were synthesized from commercially available (25R)-5-spirosten-3 beta-ol (Diosgenin) (6) as starting material. The synthesized compounds were evaluated for their antiproliferative activity, acute toxicity and effect on serum androgen level and were compared with Finasteride as positive controls. Some of the compounds exhibited better cytotoxicity and antiandrogenic activity than the reference control. The detailed synthesis, spectroscopic data and pharmacological screening for the synthesized compounds were reported.
引用
收藏
页码：2229 / 2236
页数：8
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