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.