• Patent

10,11-methylenedioxy-20(RS)-camptothecin and 10,11-methylenedioxy-20(S)-camptothecin analogs

A camptothecin analog having the structure shown below: ##STR1##where Z is H or C.sub.1-8 alkyl and R is NO.sub.2, NH.sub.2,N.sub.3, hydrogen, halogen, COOH, OH, O--C.sub.1-3 alkyl, SH,S--C.sub.1-3 alkyl, CN, CH.sub.2 NH.sub.2, NH--C.sub.1-3 alkyl,CH.sub.2 --NH--C.sub.1-3 alkyl, N(C.sub.1-3 alkyl).sub.2, CH.sub.2N(C.sub.1-3 alkyl).sub.2, O--, NH--, or S--CH.sub.2 CH.sub.2N(CH.sub.2 CH.sub.2 OH).sub.2, O--, NH-- or S-- CH.sub.2 CH.sub.2CH.sub.2 N(CH.sub.2 CH.sub.2 OH).sub.2, O--, NH-- or S--CH.sub.2CH.sub.2 N(CH.sub.2 CH.sub.2 CH.sub.2 OH).sub.2, O--, NH-- orS--CH.sub.2 CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 CH.sub.2OH.sub.2).sub.2, O--, NH-- or S--CH.sub.2 CH.sub.2 N(C.sub.1-3alkyl).sub.2, O--, NH-- or S--CH.sub.2 CH.sub.2 CH.sub.2N(C.sub.1-3 alkyl).sub.2, CHO, C.sub.1-3 alkyl or NHCOCHR.sup.1NR.sup.2 R.sup.3, where R.sup.1 is the side-chain of an.alpha.-amino acid and R.sup.2 and R.sup.3, independently arehydrogen or a lower alkyl group or R.sup.3 is a peptide unitcontaining 1-3 amino acid units bonded to the nitrogen through apeptide bond; NHCO--C.sub.2-8 -alkylene--X or NHCO--C.sub.2-8-alkenylene--X, where X is COOH; CONR.sup.2 --(CH.sub.2).sub.n--NR.sup.2 R.sup.3, where n=1-10 and R.sup.2 and R.sup.3 are asdefined above; NHCO--B--(CH.sub.2).sub.n --NR.sup.2 R.sup.3, whereB=oxygen or NH, or ##STR2## where m+y=3-6, and salts thereof.


Wall, M., Wani, M., Nicholas, A., & Manikumar, G. (1993). IPC No. U.S. 10,11-methylenedioxy-20(RS)-camptothecin and 10,11-methylenedioxy-20(S)-camptothecin analogs. (Patent No. 5180722).