are prepared from compound (III) via optical resolution of the corresponding camphanates followed by hydrolysis and acylation reactions. Key intermediate (II) is derived from known thiocolchicone (I) by ring contraction. With exception of (-)-(IVc) all compounds show strong inhibitory effects on the tubulin polymerization reaction. Compounds (II) and (-)-(IVa) also exhibit potent antitumor activity against most cell lines in NCI's in vitro screening. -(SHI, Q.; CHEN, K.; CHEN, X.; BROSSI, A.; VERDIER-PINARD, P.; HAMEL, E.; MCPHAIL, A. T.; TROPSHA, A.; LEE, K.-H.; J.
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.
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