CYCLOPROPYL AND CYCLOBUTYL EPOTHILONE ANALOGS

摘要

The invention relates to cis- and trans-12, 13-cyclopropyl and 12, 13-cyclobutyl epothilones of formula (I) to (IV), wherein Ar is a radical represented by the following structure:, and the other radicals and symbols have the meanings as defined herein; to their chemical synthesis and biological evaluation; their use in the treatment of neoplastic diseases and to pharmaceutical preparations containing such compounds. The compounds described herein are potent tubulin polymerization promoters and cytotoxic agents.