Patent ID: 6228855
Filing Date: 2001-05-08
Classification: A61P,C07D

Abstract:
An aromatic camptothecin ester having the structure: ##STR14##wherein R.sup.1 is H, NO.sub.2, NH.sub.2, N.sub.3, a halogen, carboxyl, a C.sub.1-6 alkyl group, a C.sub.1-6 alkyenyl group, a C.sub.3-8 cycloalkyl group, a C.sub.1-8 alkoxyl group, an aroxyl group, CN, SO.sub.3 H, a C.sub.1-8 halogenated alkyl group, (CH.sub.2).sub.n NR.sub.2.sup.7, hydroxyl, SH, SR.sup.8, a carbonyl group, a SiR.sub.3.sup.10 ; wherein the R.sup.1 group is respectively positioned at the 9, 10, 1 1, or 12 position of ring A; R.sup.7 is H or a C.sub.1-8 alkyl group; n is an integer of 1 to 8; R.sup.8 is a C.sub.1-8 alkyl group or a phenyl group; R.sup.10 is a C.sub.1-4 alkyl group; X is H, a C.sub.1-8 alkyl group, a C.sub.1-8 alkenyl group, a C.sub.1-8 alkoxyl group, an aroxyl group, a SiR.sub.3.sup.11 group, or CH.sub.2 NZY; and wherein R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are, independently, H, C.sub.1-12 alkyl group, C.sub.1-12 alkenyl group, COOH, SO.sub.3 H, CN, CF.sub.3, CCl.sub.3, CH.sub.2 F, CH.sub.2 Cl, CHF.sub.2, CHCl.sub.2, OH, OR.sup.12, N.sub.3, NO.sub.2, NR.sub.2.sup.13, carbonyl group, halogen, wherein R.sup.11 is a C.sub.1-4 alkyl group; Z and Y are, independently, H, C.sub.1-4 alkyl, or a C.sub.1-4 halogenated alkyl group; R.sup.12 is a C.sub.1-8 alkyl group, a C.sub.1-8 alkenyl group, or an aromatic group; and wherein R.sup.13 is H or C.sub.1-4 alkyl group, wherein at least one of R.sup.2, R.sup.3, R.sup.4, R.sup.5, or R.sup.6 is a substituent other than hydrogen, and wherein at least two of R.sup.2, R.sup.3, R.sup.4, R.sup.5, or R.sup.6 is hydrogen.