1-Hydroxy pregnacalciferol derivatives of formula (I) and their corresponding 5,6-trans isomers wherein R
1
is hydroxyl or lower alkoxy and R
2
is optionally hydroxylated or lower alkoxylated lower alkynyl or R
1
is C(R
A
) (R
B
)CH
3
where R
A
is optionally hydroxylated or lower alkoxylated lower alkynyl and R
B
is hydroxyl or lower alkoxy or R
A
and R
B
together represent oxo and R
2
is hydrogen, hydroxyl or lower alkoxy, and R
3
and R
4
represent hydrogen atoms, exhibit anti-progesterone activity and may be useful as antineoplastic, antifertility, antiproliferative, immunosuppressive and/or antiinflammatory agents.
公式(I)中的1-羟基孕
酮类衍
生物及其相应的5,6-顺式异构体,其中R1是羟基或较低的烷氧基,R2是可选择地羟化或较低烷氧化的较低炔基,或者R1是C(RA)(RB)
CH3,其中RA是可选择地羟化或较低烷氧化的较低炔基,RB是羟基或较低的烷氧基,或者RA和RB一起代表羰基,R2是氢、羟基或较低的烷氧基,R3和R4代表氢原子,表现出抗孕激素活性,可能作为抗肿瘤、抗生育、抗增殖、免疫抑制和/或抗炎药物有用。