Patent number: 6686470
Abstract: Compounds of the saframycin-ecteinascidin series with cytotoxic properties having the following general formula, their uses and synthesis, are disclosed:
wherein R1 and R4 is H, a C1 to C4 alkyl group, or an acyl group;
wherein R2 is an ether, ester, amide, or a phthalimide group; wherein R3 is ═O, OH, an ether group, an acyl group such as OC(O)Me, OC(O)Bn and OC(O)Et, or a sulfide group; wherein R5 is H, halogen, OH, an ether group, an acyl group, or an amide group; wherein R6 is ═O, OH, OCH3, CN, or an acyloxy group; wherein R7, is ═O, OH, halogen, an ether group, or an acyl group; wherein R8 and R9 are independently H, CH3, OCH3, OC2H5, CF3, halogen such as Br and F, or R8 and R9 are joined together as a methylenedioxy group, or other five or six membered ring; wherein R10 and R11 are independently CH3, OCH3, OC2H5, SCH3, or SC2H5; wherein R12 is H, a C1 to C4 alkyl group, or an acyl group; and wherein the chiral center marked * has the R or the S configuration.
Type:
Grant
Filed:
January 19, 2001
Date of Patent:
February 3, 2004
Assignee:
The Trustees of Columbia University in the City of New
York
Inventors:
Samuel J. Danishefsky, Bishan Zhou
