Enantiospecific synthesis and cytotoxicity of 7-(4-methoxyphenyl)-6-phenyl-2,3,8,8a-tetrahydroindolizin-5(1H)-one enantiomers

Enantiospecific synthesis and cytotoxicity of 7-(4-methoxyphenyl)-6-phenyl-2,3,8,8a-tetrahydroindolizin-5(1H)-one enantiomers
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DOI:
10.1016/j.bmc.2008.02.073
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发表时间:
2008-04-15
影响因子:
3.5
通讯作者:
Georg, Gunda I.
Georg, Gunda I.
中科院分区:
医学3区
文献类型:
--
作者:
Kimball, F. Scott;Turunen, Brandon J.;Georg, Gunda I.

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开发了一种对映特异性合成方法来生成 7-(4-甲氧基苯基)-6-苯基-2,3,8,8a-四氢中氮茚-5(1H)-酮的两种对映体。利用 HCT-116 结肠癌细胞系测定这些类似物的细胞毒性的生物测定表明,只有 (R)-对映异构体表现出明显的细胞毒性,IC50 值为 0.2 μM。(C) 2008 Elsevier Ltd. 保留所有权利。
An enantiospecific synthesis was developed to generate both enantiomers of 7-(4-methoxyphenyl)-6-phenyl-2,3,8,8a-tetrahydroindolizin-5(1H)-one. A biological assay utilizing the HCT-116 colon cancer cell line to determine the cytotoxicity of these analogs revealed that only the (R)-enantiomer exhibited appreciable cytotoxicity with an IC50 value of 0.2 mu M. (C) 2008 Elsevier Ltd. All rights reserved.