Antiandrogenic steroidal sulfonylpyrazoles

…, TE D'Ambra, JP Mallamo, JL Herrmann…

文献索引：Christiansen; Bell; D'Ambra; Mallamo; Herrmann; Ackerman; Opalka; Kullnig; Winneker; Snyder; Batzold; Schane Journal of Medicinal Chemistry, 1990 , vol. 33, # 8 p. 2094 - 2100

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被引用次数: 32

摘要

The steroidal sulfonylpyrazole 1 bound to the rat ventral prostate androgen receptor in vitro; it inhibited testosterone propionate induced increases in ventral prostate weight in vivo in the castrated, immature male rat with an ED, of 15 mg/kg PO. Compound 1 lacked androgenic activity in vivo in contrast to the parent steroidal pyrazole 5, which was both androgenic and antiandrogenic. The 2'-and 5'-methylsulfonyl isomers 6 and 6a did not ...