University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh 160 014, India.
Eur J Med Chem. 2010 Jun;45(6):2229-36. doi: 10.1016/j.ejmech.2010.01.064. Epub 2010 Feb 2.
The 17-oxo-17a-aza-d-homo-5-androsten-3beta-yl esters (13-22) were synthesized from commercially available (25R)-5-spirosten-3beta-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.
17-氧代-17α-氮杂-D-雄甾-5-烯-3β-基酯（13-22）是由市售的（25R）-5-螺甾-3β-醇（薯蓣皂苷元）（6）作为起始原料合成的。合成的化合物进行了抗增殖活性、急性毒性和对血清雄激素水平的影响评价，并与非那雄胺作为阳性对照进行了比较。一些化合物表现出比参考对照更好的细胞毒性和抗雄激素活性。报道了合成化合物的详细合成、光谱数据和药理学筛选。
