Synthesis and cytotoxicity of acetyl-4H,9H-naphtho[2,3-b]thiophene-4,9-diones

Bioorg Med Chem Lett. 1998 Oct 6;8(19):2763-8. doi: 10.1016/s0960-894x(98)00496-x.

Abstract

Several new acetyl-4H,9H-naphtho[2,3-b]thiophene-4,9-diones were synthesized and evaluated for in vitro cytotoxicity by NCI against seven cancer cell types. 2,7-Diacetyl naphtho[2,3-b]thiophene-4,9-dione (9) showed significant cytotoxicity against leukemia cells with log GI50 values of -7.61 against SR cells and -7.18 against MOLT-4 cells. 3-Acetyl-naphtho[2,3-b]thiophene-4,9-dione (6) also demonstrated potent cytotoxicity in the latter cell line with log GI50 < -8.

Publication types

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

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology*
  • Drug Screening Assays, Antitumor
  • Humans
  • KB Cells / drug effects
  • Naphthols / chemical synthesis*
  • Naphthols / pharmacology*
  • Nuclear Magnetic Resonance, Biomolecular / methods
  • Thiophenes / chemical synthesis*
  • Thiophenes / pharmacology*
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents
  • Naphthols
  • Thiophenes