ChemInform Abstract: Antitumor Agents. Part 184. Syntheses and Antitubulin Activity of Compounds Derived from Reaction of Thiocolchicone with Amines: Lactams, Alcohols, and Ester Analogues of Allothiocolchicinoids.

Abstract

Allothiocolchicinoids. -Racemic title compounds such as (V) are synthesized and resolved by reaction with (-)-camphanic chloride to the (7R)-and (7S)-enantiomers. All compounds are evaluated for their inhibitory effects on tubulin polymerization in vitro. Some of the most active compounds are (II), (7S)-(Va) and the (7R)-(Vb). -(SHI, Q.; CHEN, K.; BROSSI, A.; VERDIER-PINARD, P.; HAMEL, E.; MCPHAIL, A. T.; LEE, K.-H.; Helv.