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用于对HCT - 116结肠癌细胞系进行细胞毒性研究的杂芳基6,7 - 二芳基 - 2,3,8,8a - 四氢中氮茚 - 5(1H) - 酮的合成与评价

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.

作者信息

Kimball F Scott, Himes Richard H, Georg Gunda I

机构信息

Department of Medicinal Chemistry, University of Kansas, 1251 Wescoe Hall Drive, Lawrence, KS 66045, USA.

出版信息

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3248-50. doi: 10.1016/j.bmcl.2008.04.051. Epub 2008 Apr 25.

DOI:10.1016/j.bmcl.2008.04.051
PMID:18479919
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2475576/
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 IC(50) values of 0.27 microM and 0.60 microM, respectively.

摘要

制备了一个杂芳基6,7-二芳基-2,3,8,8a-四氢中氮茚-5(1H)-酮类似物库，并测试了其对HCT-116结肠癌细胞系的细胞毒性，从而提供了有关这类化合物构效关系的更多信息。新类似物中活性最高的是C6 2-噻吩和3-噻吩类似物，其IC(50)值分别为(0.27)微摩尔和(0.60)微摩尔。

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本文引用的文献

1
Enantiospecific synthesis and cytotoxicity of 7-(4-methoxyphenyl)-6-phenyl-2,3,8,8a-tetrahydroindolizin-5(1H)-one enantiomers.
Bioorg Med Chem. 2008 Apr 15;16(8):4367-77. doi: 10.1016/j.bmc.2008.02.073. Epub 2008 Mar 4.
2
Synthesis, in vitro and in vivo cytotoxicity of 6,7-diaryl-2,3,8,8a-tetrahydroindolizin-5(1H)-ones.
Bioorg Med Chem Lett. 2007 Aug 15;17(16):4703-7. doi: 10.1016/j.bmcl.2007.05.103. Epub 2007 Jun 13.
3
Novel 6,7-diphenyl-2,3,8,8a-tetrahydro-1H-indolizin-5-one analogues as cytotoxic agents.
Bioorg Med Chem Lett. 2003 May 19;13(10):1679-82. doi: 10.1016/s0960-894x(03)00263-4.
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Cytotoxic alkaloids from Tylophora indica.
Pharmazie. 2001 Feb;56(2):188-90.

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