Molecular modifications of 2-arylidene-1-indanones leading to increased cytotoxic potencies

Molecular modifications of 2-arylidene-1-indanones leading to increased cytotoxic potencies
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DOI:
10.1080/14756360600958057
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发表时间:
2007-02-01
影响因子:
5.6
通讯作者:
Dimmock, Jonathan R.
Dimmock, Jonathan R.
中科院分区:
医学2区
文献类型:
--
作者:
Pati, Hari N.;Das, Umashankar;Dimmock, Jonathan R.

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此前已有研究表明,一系列2-亚芳基-1-吲哚类化合物对Molt 4/C8、CEM和L1210细胞具有细胞毒作用。本研究合成了1的两个系列的类似物,即各种2-亚芳基-1,3-吲二酮类化合物2和查尔酮类化合物3。一般来说,化合物2和3的势能大于系列1中含有相同芳基取代基的类似物。为了寻求生物活性变化的原因,进行了分子模拟。
A series of 2-arylidene-1-indanones, 1, had been shown previously to display cytotoxic properties towards Molt 4/C8, CEM and L1210 cells. In the present study, two series of analogues of 1 were prepared namely various 2-arylidene- 1,3-indandiones, 2, and chalcones, 3. In general, the potencies of compounds 2 and 3 were greater than the analogues bearing the same aryl substituents in series 1. Molecular modeling was undertaken in order to seek explanations for the variation in bioactivities.