2-substituted pregna-1,3,5(10)-triene and chola-1,3,5(10)-triene derivatives and their biological activity.

摘要

Compounds of formula (I) in which: R<1> represents a hydrogen atom or an O-protecting group; R<2> represents a hydroxyl, lower alkoxy, carboxaldehyde, lower alk-1-enyl or hydroxy- or lower alkoxy-substituted lower alkyl group; R<3> represents a methyl group having alpha - or beta - configuration; X represents a C1-3 alkylene group or a valence bond; Y represents a carboxaldehyde group or a group of formula -C(R<4>) (R<5>)OR<1> where R<1> is as defined above and R<4> and R<5>, which may be the same or different, are each selected from hydrogen atoms, alkyl, alkenyl and alkynyl groups such that the total carbon content of R<4> and R<5> does not exceed three atoms, with the proviso that X is a valence bond when both R<4> and R<5> are other than hydrogen; and the dotted line signifies that a double bond may optionally be present at the 16(17) -position exhibit potent cell modulating activity, including antiproliferative and antiangiogenic effects.