Synthesis, in vitro and in vivo cytotoxicity of 6,7-diaryl-2,3,8,8a-tetrahydroindolizin-5(1H)-ones

F. Scott Kimball, Ashok Rao Tunoori, Samuel F. Victory, Dinah Dutta, Jonathan M. White, Richard H. Himes, Gunda I. Georg

Research output: Contribution to journalArticlepeer-review

18 Scopus citations

Abstract

A 6,7-diaryl-2,3,8,8a-tetrahydroindolizin-5(1H)-one library was constructed and tested against the colon cancer cell line HCT-116 as an initial screen for cytotoxic properties. Of this library, the parent compound, in which the southern aromatic ring remains unsubstituted, and the northern aromatic ring carries a 4-methoxy group, exhibited the most potent cytotoxicity with an IC50 value of 0.39 μM and displayed promising activity in vivo in the NCI's mouse hollow fiber assay.

Original languageEnglish (US)
Pages (from-to)4703-4707
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume17
Issue number16
DOIs
StatePublished - Aug 15 2007
Externally publishedYes

Bibliographical note

Funding Information:
These studies were supported by the National Cancer Institute (CA 90602 and N01-CM-67259). The authors thank Dr. Ravi Varma (NCI, DTP) for carrying out the COMPARE analysis for analog 12 (NSC 707904) and for his support of this project. We also wish to thank the NCI’s DTP for carrying out cytotoxicity assays for compounds 12 (NSC 707904), 14 (NSC 707907), and 27 (NSC 707909). The complete cancer screening data for these compounds are available on the DTP website.

Keywords

  • COMPARE analysis
  • Colon cancer
  • HCT-116
  • NCI mouse hollow fiber assay
  • Seco-phenanthroindolizidine alkaloids

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