These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Design, synthesis and anticancer properties of IsoCombretaQuinolines as potent tubulin assembly inhibitors.
    Author: Khelifi I, Naret T, Renko D, Hamze A, Bernadat G, Bignon J, Lenoir C, Dubois J, Brion JD, Provot O, Alami M.
    Journal: Eur J Med Chem; 2017 Feb 15; 127():1025-1034. PubMed ID: 28166995.
    Abstract:
    The synthesis and evaluation of a new series of IsoCombretaQuinolines (IsoCoQuines) 2 with a 2-substituted-quinoline in place of the 3,4,5-trimethoxyphenyl ring present in isoCA-4 and CA-4 are described. Most of these compounds displayed a potent cytotoxic activity (IC50 < 10 nM) against a panel of five human cancer cell lines and inhibited tubulin assembly at a micromolar level. The most potent analogue 2b, having a 3-hydroxy-4-methoxyphenyl as B-ring, led to cell cycle arrest in G2/M phase. Docking studies indicate that 2b showed a binding mode comparable to those previously observed with quinazoline analogous (IsoCoQ) and with isoCA-4 at the colchicine binding site of tubulin.
    [Abstract] [Full Text] [Related] [New Search]