Synthesis, antiproliferative, acute toxicity and assessment of antiandrogenic activities of some newly synthesized steroidal lactams
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- 作者：Neelima Dhingra ; T.R. Bhardwaj ; Neeraj Mehta ; Tapas Mukhopadhyay ; Ashok Kumar ; Manoj Kumar
- 关键词：Dihydrotestosterone ; Five alpha reductase enzyme ; Benign prostatic hyperplasia ; 17a-Aza steroids ; Androgen
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2010
- 出版时间：June 2010
- 年：2010
- 卷：45
- 期：6
- 页码：2229-2236
- 全文大小：556 K
文摘
The 17-oxo-17a-aza-d-homo-5-androsten-3β-yl esters (13–22) were synthesized from commercially available (25R)-5-spirosten-3β-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.