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 μM.
Indole derivatives as tubulin polymerization inhibitors and their preparation and use for the treatment of cancer / Silvestri, Romano; LA REGINA, Giuseppe; Hamel, E.; Brancale, A.; Lavia, P.; Novellino, E.. - (2011).
Indole derivatives as tubulin polymerization inhibitors and their preparation and use for the treatment of cancer.
SILVESTRI, Romano;LA REGINA, GIUSEPPE;
2011
Abstract
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 μM.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
