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三取代-1,3,5-三嗪的合成与细胞毒性活性

Synthesis and cytotoxic activity of trisubstituted-1,3,5-triazines.

作者信息

Arya Kapil, Dandia Anshu

机构信息

Indian Oil Corporation Limited, R&D Center, Faridabad, Haryana 121007, India.

出版信息

Bioorg Med Chem Lett. 2007 Jun 15;17(12):3298-304. doi: 10.1016/j.bmcl.2007.04.007. Epub 2007 Apr 10.

DOI:10.1016/j.bmcl.2007.04.007
PMID:17449247
Abstract

1,3,5-Triazine derivatives were screened for phototoxicity as well as the cytotoxic activities against leukemia and adenocarcinoma derived cell lines in comparison to the normal human keratinocytes. A simple and environmentally friendly procedure has been developed for the synthesis of 1,3,5-triazine derivatives under microwave irradiation in the presence of a HY zeolite. The catalyst can be recovered and reused. Thus, the procedure provides a simple and green synthetic methodology under environmentally friendly conditions. Structure-activity relationships between the chemical structures and antimycobacterial and photosynthesis-inhibiting activity of the evaluated compounds are also discussed.

摘要

对1,3,5-三嗪衍生物进行了光毒性筛选,并与正常人角质形成细胞相比,评估了其对白血病和腺癌衍生细胞系的细胞毒性活性。已经开发出一种简单且环境友好的方法,用于在HY沸石存在下微波辐射合成1,3,5-三嗪衍生物。该催化剂可回收再利用。因此,该方法在环境友好条件下提供了一种简单且绿色的合成方法。还讨论了所评估化合物的化学结构与抗分枝杆菌及光合作用抑制活性之间的构效关系。

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