Quinoxaline chemistry. Part 8. 2-[Anilino]-3-[carboxy]-6(7)-substituted quinoxalines as non classical antifolate agents. Synthesis and evaluation of in vitro anticancer, anti-HIV and antifungal activity

Farmaco. 1997 Aug-Sep;52(8-9):531-7.

Abstract

Thirty quinoxalines bearing a substituted anilino group on position 2, a carboethoxy or carboxy group on position 3 and a trifluoromethyl group on position 6 or 7 of the heterocycle were prepared in order to evaluate in vitro anticancer activity. Preliminary screening performed at NCI showed that most derivatives exhibited a moderate to strong growth inhibition activity on various tumor panel cell lines between 10(-5) and 10(-4) molar concentrations. Interesting selectivities were also recorded between 10(-8) and 10(-6) M for a few compounds. One single compound exhibited good activity against Candida albicans.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / chemical synthesis
  • Anti-HIV Agents / pharmacology
  • Antifungal Agents / chemical synthesis
  • Antifungal Agents / pharmacology
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / pharmacology
  • Candida albicans
  • Drug Screening Assays, Antitumor
  • Folic Acid Antagonists / chemical synthesis*
  • Folic Acid Antagonists / pharmacology
  • Humans
  • Microbial Sensitivity Tests
  • Quinoxalines / chemical synthesis*
  • Quinoxalines / pharmacology

Substances

  • Anti-HIV Agents
  • Antifungal Agents
  • Antineoplastic Agents
  • Folic Acid Antagonists
  • Quinoxalines