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微波辅助合成N-取代环状酰亚胺及其抗癌和抗炎活性评价。

Microwave-assisted synthesis of N-substituted cyclic imides and their evaluation for anticancer and anti-inflammatory activities.

作者信息

Sondhi Sham M, Rani Reshma, Roy Partha, Agrawal S K, Saxena A K

机构信息

Department of Chemistry, Indian Institute of Technology-Roorkee, Roorkee, Uttaranchal 247667, India.

出版信息

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1534-8. doi: 10.1016/j.bmcl.2008.07.048. Epub 2008 Jul 17.

Abstract

A number of N-substituted cyclic imides 3a-e, 5a-e, 7a-d, and 9a-e have been synthesized in very high yields, by condensation of various diacids 2, 4, 6, and 8 with different amines under microwave irradiation. These compounds were screened for anticancer and anti-inflammatory activities, and compounds 3c, 3e, 5c, 9c, and 9d exhibited anticancer activity against colon (COLO 205) cancer better than 5-fluorouracil and mitomycin-C, and compound 9b exhibited anti-inflammatory activity better than standard drug phenyl butazone.

摘要

通过在微波辐射下使各种二酸2、4、6和8与不同的胺缩合,已以非常高的产率合成了许多N-取代的环状酰亚胺3a-e、5a-e、7a-d和9a-e。对这些化合物进行了抗癌和抗炎活性筛选,化合物3c、3e、5c、9c和9d对结肠癌(COLO 205)的抗癌活性优于5-氟尿嘧啶和丝裂霉素-C,化合物9b的抗炎活性优于标准药物保泰松。

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