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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.

✍ Scribed by Q. SHI; K. CHEN; A. BROSSI; P. VERDIER-PINARD; E. HAMEL; A. T. MCPHAIL; K.-H. LEE

Publisher: John Wiley and Sons
Year: 2010
Weight: 32 KB
Volume: 29
Category: Article
ISSN: 0931-7597
DOI: 10.1002/chin.199834257

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✦ Synopsis

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