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

doi:10.1016/j.bmcl.2008.04.051

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

Medicinal Chemistry

Research output: Contribution to journal › Article › peer-review

6 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 language	English (US)
Pages (from-to)	3248-3250
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	11
DOIs	https://doi.org/10.1016/j.bmcl.2008.04.051
State	Published - 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.

Keywords

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

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title = "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",

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.",

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author = "{Scott Kimball}, F. and Himes, {Richard H.} and Georg, {Gunda I.}",

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.",

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AU - Scott Kimball, F.

AU - Himes, Richard H.

AU - Georg, Gunda I.

N1 - 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.

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KW - Cytotoxicity

KW - HCT-116 colon cancer cell line

KW - Heteroaromatic

KW - Structure-activity studies

KW - Synthesis

KW - Tetrahydroindolizinones

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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

Abstract

Bibliographical note

Keywords

UN SDGs

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