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.

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.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
  • Anti-HIV Agents / chemical synthesis
  • Anti-HIV Agents / pharmacology
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology*
  • HIV Infections / drug therapy
  • HIV Infections / virology
  • Humans
  • Lymphocytes / drug effects
  • Lymphocytes / virology
  • Quinazolines / chemical synthesis*
  • Quinazolines / pharmacology*
  • Structure-Activity Relationship
  • Tubulin / biosynthesis
  • Tubulin / drug effects
  • Tumor Cells, Cultured

Substances

  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • Anti-HIV Agents
  • Antineoplastic Agents
  • Quinazolines
  • Tubulin