The invention relates to indole derivs. of formula I, which are tubulin polymn. inhibitors and which are useful in the treatment of cancer. Compds. of formula I wherein R1 is (un)substituted Ph and (un)substituted (un)fused heterocycle; R2 is attached to one or more positions and each R2 is independently H, alkyl, C2-6 alkenyl, etc.; X is S, SO, SO2, CO, etc.; provided that when X is CO, S, SO and SO2, R2 at position 6 is not methoxy; are claimed. Example compd. II was prepd. by thioetherification and in situ deprotection of 2-[1-(phenylsulfonyl)-1H-pyrrol-3-yl]-1H-indole with bis(3,4,5-trimethoxyphenyl)disulfide. All the invention compds. were evaluated for their tubulin polymn. inhibitory activity. From the assay, it was detd. that compd. II exhibited an IC50 value of 1.2 ± 0.2 microM.
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|Titolo:||Indole derivatives as tubulin polymerization inhibitors and their preparation and use for the treatment of cancer|
|Anno di primo deposito:||2013|
|Appartiene alla tipologia:||05a Brevetto|