New thio derivatives of gossypol or gossypolone, useful as anticancer agents, particularly for the treatment of solid tumors, or as intermediates in the synthesis of new gossypol or gossypolone derivatives

摘要

New gossypol derivatives (I) comprise thio derivatives (especially 1,3-dithiolan or 1,3-dithian derivatives) of gossypol, gossypolone or gossypol methyl ethers. Gossypol derivatives of formula (I), preferably of formula (Ia) or (Ib), are new. A = O (in which case bonds d and f are double and bond e is single) or OH (in which case bonds d and f are single and bond e is double); W = when n2 = 0, W represents the functionality present in (Ia); or when n2 = 1, W represents the functionality present in (Ib); n2 = 0-1; n = 2-5 (preferably 2 or 3); Y = C-OH and Z' = CH (in which case bonds a and c are double and bond b is single); or Y, Z' = CO (in which case bonds a and c are single and bond b is double); R1 - R4 = H or 1-3C alkyl (preferably Me). Independent claims are also included for: (1) New compounds (I') comprising (I) bonded (optionally via a spacer) to a polymer (II) showing trophism for tumors; and (2) Preparation of (I).