Synthesis of indole-derived allocolchicine congeners exhibiting pronounced anti-proliferative and apoptosis-inducing properties. Issue 12 (30th October 2015)

• Record Type: Journal Article
• Authors: Sitnikov, Nikolay S.; Sinzov, Alexander V.; Allegro, Diane; Barbier, Pascale; Combes, Sebastien; Onambele, Liliane Abodo; Prokop, Aram; Schmalz, Hans-Günther; Fedorov, Alexey Yu.
• Is Part Of: MedChemComm. Volume 6:Issue 12(2015:Dec.)
• Page Start: 2158
• Page End: 2162
• Publication Date: 2015-10-30
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19
• DOI: 10.1039/c5md00320b
• Languages: English
• ISSNs: 2040-2503

Abstract

Abstract : The synthesis and biological assessment of indole-based allocolchicine congeners with potent anti-proliferative and apoptosis-inducing activity are reported. Abstract : Based on the natural antimitotic agent allocolchicine as a lead structure, a series of novel indole-based allocolchicine congeners was synthesized and assessed in vitro for their cytostatic properties. Several compounds exhibited potent anti-proliferative and apoptosis-inducing activity towards lymphoma cells along with low unspecific cytotoxicity. The observed activity is supposed to result from the inhibition of microtubule assembly, as indicated by the tubulin polymerisation assay.