Studies on indolizines. Evaluation of their biological properties as microtubule-interacting agents and as melanoma targeting compounds.
Basic Information
ID: ALA3352214
Journal: Eur J Med Chem
Title: Studies on indolizines. Evaluation of their biological properties as microtubule-interacting agents and as melanoma targeting compounds.
Authors: Ghinet A, Abuhaie CM, Gautret P, Rigo B, Dubois J, Farce A, Belei D, Bîcu E.
Abstract: With the aim of investigating new analogues of phenstatin with an indolizin-3-yl unit, in particular as the B-ring, three new series of compounds (6-8, 9-34 and 54) were synthesized and tested for interactions with tubulin polymerization and evaluated for cytotoxicity on an NCI-60 human cancer cell lines panel. The replacement of the 3'-hydroxy-4'-methoxyphenyl B-ring of phenstatin with substituted indolizine unit results in the conservation of both antitubulin and cytotoxic effect. Indolizines 9 and 17 were the most effective in the present study and showed the highest antiproliferative effect on melanoma cell lines MDA-MB-435 (GI50 = 30 nM) and could serve as new lead compounds for the development of anti-cancer therapeutics.
CiteXplore: 25462232
DOI: 10.1016/j.ejmech.2014.10.041
Patent ID: ┄