Steroids p. 803 - 810 (2001)
Update date:2022-08-04
Topics: Mechanism of Action Substrate
Grisenti
Magni
Olgiati
Manzocchi
Ferraboschi
Villani
Pucciariello
Celotti
A series of steroidal compounds were synthesized in order to evaluate the possible influence of the configuration of a stereocenter in the 17beta-side chain on the inhibitory activity on the enzyme 5alpha-reductase (5AR). For this purpose diastereomerically pure 4-azasteroids epimers at C-22 were prepared (compounds 1-11) and tested as inhibitors of 5AR in "in vitro" tests. The obtained data showed that in most cases the couples of epimers possess a significant difference in their biological activity. We also considered, for the tested molecules, a series of chemico-physical parameters in order to find a possible correlation with their biological activity. The findings allowed us to propose a model of the binding site of 5AR which comprises also, for 4-azasteroid inhibitors, the configurational aspect of the 17beta-side chain.
View MoreGuangzhou Probig Fine Chemical Co., Ltd.
Contact:020-86297874
Address:No.2, 1/F, No.20, Hetai Road,Hebian Village, Baiyun District,Guangzhou,China
website:http://www.shengmaochem.com
Contact:86-27-82853423, 82819281
Address:Rm 202, A Unit Huaqiao Building No. 2, Lihuangpi Road, Wuhan, China
Shantou Baokang Pharmaceutical Co., Ltd.
Contact:+86-754-88873487
Address:5/F B Block Huangshan Bldg Huangshan Rd Shantou
Contact:86-513-84128750/13773795976
Address:No.48.Youyi West Road ,Rudong Development Zone,Jiangsu Province,China
Xiamen Kaijia Imp & Exp Co., Ltd.
Contact:86-592-5101177
Address:Room406 Luhui Building No. 65 Haitian Road Huli Xiamen,China.
Doi:10.1080/10610278.2018.1494275
(2018)Doi:10.1021/ja01329a040
(1933)Doi:10.1021/ol016960n
(2001)Doi:10.1007/BF00846201
()Doi:10.1016/S0022-328X(00)82916-2
(1972)Doi:10.1021/j100243a036
(1983)