| abstract |
A taxane derivative of the formula (see fig. 3) wherein R1 is phenyl or substituted phenyl, R3 is CH3O-, or CH3CH2O-, Z is -OCOT2, T2 is H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or monocycllc aryl, Ac is acetyl, and E1 and E2 are independently selected from hydrogen, and functional groups which increase the water solubility of the taxane derivative, the functional groups having the formula -COGCOR1 wherein: G is ethylene, propylene, CHCH, 1,2-cyclo-hexylene, or 1,2-phenylene; R1 = OH base, NR2R3, OR3, SR3, OCH2CONR4R5, or OH; R2 = hydrogen or methyl; R3 = (CH2)nNR6R7 or (CH2)nNR+6R7R8X-; n = 1 to 3 R6 and R7 = independently selected from lower alkyl containing 1 or 2 carbons, or benzyl, or R6 and R7 together with the nitrogen atom of NR6R7 forms one of the following rings (see fig. 4) or (see fig. 5); R8 = lower alkyl containing 1 or 2 carbons or benzyl; Xe = halide; and base = NH3, (HOC2H4)3N, N(CH3)3, CH3N(C2H4OH)2, NH2(CH2)6NH2, N-methylglucamine, NaOH, or KOH, are useful as antitumor agents. |