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.
Bibliographical noteFunding 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 2008 Elsevier B.V., All rights reserved.
- HCT-116 colon cancer cell line
- Structure-activity studies