HIGHLY LIPOPHILIC CAMPTOTHECIN DERIVATIVES

摘要

Novel camptothecin compounds having the general formula: (see formula I) wherein: R1 is selected from: acyl, C2-C8 alkenyl, or C2-C8 alkynyl, optionally substituted by one or more halogen atoms or OR9 or lower alkyl for a corresponding hydrogen atom therein; oxo; arylalkenyl; arylalkynyl; heterocycle; -S(O)-lower alkyl; and -lower alkyl-P (O) R6R, or -X- (C0-C6 alkyl , C0-C9 alkenyl , or C0-C8 alkynyl) -SiR8R9R10; R2 is hydrogen, halo, lower alkyl, amino or nitro; R4 is hydrogen or lower alkyl; R6 and R7 are each individually hydrogen or lower alkyl; R8, R9 and R10 are each individually hydrogen or lower alkyl; R11 is hydrogen, hydroxy or acetoxy; and X is sulfur or X is absent. The invention also includes the use of these compounds as Topoisomerase I inhibitors to treat patients with cancer. The invention also includes pharmaceutical compositions which consist of the novel compounds in solution or suspension with one or more pharmaceutical acceptable carriers.