Synthesis and evaluation of heteroaromatic 6,7-diaryl-2,3,8,8a-tetrahydroindolizin-5(1H)-ones for cytotoxicity against the HCT-116 colon cancer cell line

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3248-50. doi: 10.1016/j.bmcl.2008.04.051. Epub 2008 Apr 25.

Abstract

A heteroaromatic 6,7-diaryl-2,3,8,8a-tetrahydroindolizin-5(1H)-one analog library was prepared and tested for cytotoxic properties against the HCT-116 colon cancer cell line, thus providing additional information pertaining to structure-activity relationships for this class of compounds. The most active of the new analogs proved to be the C6 2-thiophene and 3-thiophene analogs with IC(50) values of 0.27 microM and 0.60 microM, respectively.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • HCT116 Cells
  • Humans
  • Indolizines / chemical synthesis*
  • Indolizines / chemistry
  • Indolizines / pharmacology*
  • Inhibitory Concentration 50
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Indolizines