Issue 12, 2015
From the journal:

MedChemComm

Synthesis of indole-derived allocolchicine congeners exhibiting pronounced anti-proliferative and apoptosis-inducing properties†

Nikolay S. Sitnikov,ab   Alexander V. Sinzov,a   Diane Allegro,c   Pascale Barbier,c   Sebastien Combes,d   Liliane Abodo Onambele,e   Aram Prokop,e   Hans-Günther Schmalzb  and  Alexey Yu. Fedorov*a  

* Corresponding authors

a Department of Organic Chemistry, Lobachevsky State University of Nizhni Novgorod, Gagarina Av. 23, Nizhni Novgorod 603950, Russia
E-mail: afnn@rambler.ru

b Department für Chemie, Universität zu Köln, Greinstr. 4, Köln, Germany

c Aix-Marseille Université, INSERM, CRO2 UMR_S 911, Marseille, France

d Laboratory of Integrative Structural and Chemical Biology, Institut Paoli-Calmettes, Aix-Marseille Université, UM 105, Marseille, France

e Department of Pediatric Hematology/Oncology, Children's Hospital Köln, Amsterdamer Str. 59, 50735 Köln, Germany

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.

Graphical abstract: Synthesis of indole-derived allocolchicine congeners exhibiting pronounced anti-proliferative and apoptosis-inducing properties

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Article information

DOI
https://doi.org/10.1039/C5MD00320B
Article type
Concise Article
Submitted
04 Aug 2015
Accepted
20 Sep 2015
First published
22 Sep 2015
This article is Open Access
Creative Commons BY license

Med. Chem. Commun., 2015,6, 2158-2162

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Synthesis of indole-derived allocolchicine congeners exhibiting pronounced anti-proliferative and apoptosis-inducing properties

N. S. Sitnikov, A. V. Sinzov, D. Allegro, P. Barbier, S. Combes, L. A. Onambele, A. Prokop, H. Schmalz and A. Yu. Fedorov, Med. Chem. Commun., 2015, 6, 2158 DOI: 10.1039/C5MD00320B

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