Antitumor agents. Part 204: synthesis and biological evaluation of substituted 2-aryl quinazolinones

  • Bioorg Med Chem Lett. 2001 May 7;11(9):1193-6. doi: 10.1016/s0960-894x(01)00190-1.
Y Xia  1 ,  Z Y Yang ,  M J Hour ,  S C Kuo ,  P Xia ,  K F Bastow ,  Y Nakanishi ,  P Namrpoothiri ,  T Hackl ,  E Hamel ,  H K Lee
Affiliations
  • 1. Natural Products Laboratory, School of Pharmacy, University of North Carolina, Chapel Hill 27599, USA.
PMID: 11354375 DOI: 10.1016/s0960-894x(01)00190-1
Abstract

A series of 2',3',4',6,7-substituted 2-aryl quinazolinones were synthesized and evaluated for biological activity. Among them, 17 displayed significant growth inhibitory action against a panel of tumor cell lines. Compound 17 was also a potent inhibitor of tubulin polymerization. Compounds 8-10 displayed selective activity against P-gp-expressing epidermoid carcinoma of the asopharynx.