CA2116621C — Novel anticancer agents

USPTO Abstract

The present invention is concerned with novel anticancer agents having potent antineoplastic activity without systemic toxicity and mutagenicity. The novel anticancer agents of the present invention are derivatives of formula I: (see formula I) wherein: A is O or NH; and B is an aryl group selected from the group consisting of phenyl, indane, fluorene, indazole, indole, and pyridine, the aryl group being substituted with at least one substituent selected from the group consisting of hydrogen, C1-16 alkyl optionally substituted with one or more OH or SH, lower alkoxy, C3-6 cycloalkyl, lower alkylthio, nitro, cyano, lower alkene, lower alkyne, OH, SH, carboxy lower alkyl, carboxy lower alkyl esters, amino, N-lower alkyl, N,N-dilower alkyl and halogen; or a prodrug thereof, with the provisos that when A is NH and B is phenyl: a) B is substituted with at least one substituent other than hydrogen; b) B is not: 1) mono-substituted in the 4 position with C1-2 alkyl, tert-butyl or n-butyl, halogen, OH, carboxy C0-3 alkyl, (CH2)3COOCH3, cyano, acetyl and methylthio; and 2) substituted with one or two identical substituents selected from the group consisting of methyl, halogen, nitro, methoxy, carboxy and C0-3alkyl COON, the remaining substituents being hydrogen atoms.