Discovery of indolizines containing triazine moiety as new leads for the development of antitumoral agents targeting mitotic events. Issue 18 (15th September 2015)

• Record Type: Journal Article
• Authors: Lucescu, Liliana; Ghinet, Alina; Belei, Dalila; Rigo, Benoît; Dubois, Joëlle; Bîcu, Elena
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 18(2015)
• Page Start: 3975
• Page End: 3979
• Publication Date: 2015-09-15
• Subjects: Indolizine -- Dimethoxytriazine -- Antitumor agent -- PLK1 -- Polo-like kinase 1 inhibitor -- O-demethylation -- Hilbert–Johnson transposition; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.07.025
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A new family of 3-aroylindolizines bearing a dimethoxytriazine unit in their position 1 was designed, synthesized and evaluated for their ability to inhibit tubulin polymerization and cellular growth in vitro. Compound39 was the best candidate in the current study with a GI50 value of 870 nM on SNB-75 CNS cancer cells and of 920 nM on MDA-MB-231/ATCC breast cancer cells. The standard NCI Compare results indicated that indolizine39 may target PLK1 (polo-like kinase 1).