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

F. Scott Kimball, Richard H. Himes, Gunda I. Georg

Research output: Contribution to journalArticlepeer-review

5 Scopus citations

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 IC50 values of 0.27 μM and 0.60 μM, respectively.

Original languageEnglish (US)
Pages (from-to)3248-3250
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number11
DOIs
StatePublished - Jun 1 2008

Bibliographical note

Funding Information:
These studies were supported by the National Cancer Institute (CA 90602 and N01-CM-67259). We thank Deborah A. Bohlander for conducting the cytotoxicity assays.

Copyright:
Copyright 2008 Elsevier B.V., All rights reserved.

Keywords

  • Cytotoxicity
  • HCT-116 colon cancer cell line
  • Heteroaromatic
  • Structure-activity studies
  • Synthesis
  • Tetrahydroindolizinones

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