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

A heteroaromatic 6,7-diaryl-2,3,8,8a-tetrahydroindolizin-5(1 H)-one library was prepared and tested for cytotoxic properties against the HCT-116 colon cancer cell line, thus providing information pertaining to structure–activity relationships for this class of compounds. The most active of the new a...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2008-06, Vol.18 (11), p.3248-3250
Hauptverfasser: Scott Kimball, F., Himes, Richard H., Georg, Gunda I.
Format: Artikel
Sprache:eng
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Zusammenfassung:A heteroaromatic 6,7-diaryl-2,3,8,8a-tetrahydroindolizin-5(1 H)-one library was prepared and tested for cytotoxic properties against the HCT-116 colon cancer cell line, thus providing 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 an IC 50 values of 0.27 μM and 0.60 μM, respectively. A heteroaromatic 6,7-diaryl-2,3,8,8a-tetrahydroindolizin-5(1 H)-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 μM and 0.60 μM, respectively.
ISSN:0960-894X
0968-0896
1464-3405
1464-3391
DOI:10.1016/j.bmcl.2008.04.051