10,11-methylenedioxy-20(rs)-camptothecin and...

Details 10,11-methylenedioxy-20(rs)-camptothecin and... 10,11-methylenedioxy-20(rs)-camptothecin and...

C - Chemistry, Metallurgy

07

D

C07D 491/22 (2006.01) A61K 31/47 (2006.01) A61K 31/495 (2006.01) A61K 38/04 (2006.01) C07K 5/04 (2006.01)

Patent

CA 2066780

A camptothecin analog having structures (I) or (II), where Z is H or C1-8 alkyl and R is NO2, NH2, N3, hydrogen, halog- en, COOH, OH, O-C1-3 alkyl, SH, S-C1-3 alkyl, CN, CH2NH2, NH-C1-3 alkyl, CH2- NH-C1-3 alkyl, N(C1-3 alkyl)2, CH2N(C1-3 alkyl)2, O-, NH- or S-CH2CH2N(CH2CH2OH)2, O-, NH- or S- CH2CH2CH2N(CH2CH2OH)2, O-, NH- or S- CH2CH2N(CH2CH2CH2OH)2, O-, NH- or S-CH2CH2CH2N(CH2CH2CH2OH2)2, O-, NH- or S- CH2CH2N(C1-3 alkyl)2, O-, NH- or S-CH2CH2CH2N(C1-3 alkyl)2, CHO, C1-3 alkyl or NHCOCHR1NR2R3, where R1 is the side-chain of an .alpha.-ami- no acid and R2 and R3, independently are hydrogen or a lower alkyl group or R3 is a peptide unit containing 1-3 amino acid units bonded to the nitrogen through a peptide bond; NHCO-C2-8-alkylene-X or NHCO-C2-8-alkenylene-X, where X is COOH; CONR2-(CH2)n-NR2-R3, where n = 1-10 and R2 and R3 are as defined above; NHCO-B-(CH2)n-NR2R3, where B = oxygen or NH, or structure (III), where m + y = 3-6, and salts thereof.

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