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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis and Biological Evaluation of Some New Indolizine Derivatives as Antitumoral Agents

Author(s): Liliana Lucescu, Elena Bîcu, Dalila Belei, Joelle Dubois and Alina Ghinet

Volume 13, Issue 6, 2016

Page: [479 - 488] Pages: 10

DOI: 10.2174/1570180812666151022221628

Price: $65

Abstract

A new series of indolizine derivatives were synthesized and screened for the antiproliferative potential against NCI 60 tumor cell line panel. The results of the study revealed a selective and good antitumor growth inhibitory activity against SNB-75 CNS cancer cell line for 1-cyanoindolizine derivative 10b. Moreover, a supplementary in vitro biological evaluation showed that compound 9d exhibited a significant farnesyltransferase inhibition activity (IC50 = 1.07 ± 0.34 µM) and could represent a lead for the development of new antitumoral chemical entities.

Keywords: Indolizine, farnesyltransferase, anticancer agent.

Graphical Abstract


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