Synthesis and biological evaluation of cyanoguanidine derivatives of loratadine.

Wukun Liu, Jinpei Zhou, Tong Zhang, Huibin Zhang, Haiyang Zhu, Yanhua Cheng, Ronald Gust

Department of Medicinal Chemistry, China Pharmaceutical University, Tongjia Xiang 24, 210009 Nanjing, PR China.

Bioorganic & medicinal chemistry letters 2012 Oct 1

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Cyanoguanidine derivatives of loratadine (3a-i) were synthesized and screened for antitumor and anti-inflammatory activity. The most promising compound 3c (R=n-C(8)H(17)) possessed at least twofold higher in vitro cytotoxicity than 5-fluorouracil against mammary (MCF-7 and MDA-MB 231) as well as colon (HT-29) carcinoma cells. The mode of action, however, is so far unclear. The participation of the COX-1/2 enzymes on the cytotoxicity, however, is very unlikely. Nevertheless all compounds showed stronger in vivo anti-inflammatory activity than ibuprofen in the xylene-induced ear swelling assay in mice. Copyright © 2012 Elsevier Ltd. All rights reserved.

Citation

Wukun Liu, Jinpei Zhou, Tong Zhang, Huibin Zhang, Haiyang Zhu, Yanhua Cheng, Ronald Gust. Synthesis and biological evaluation of cyanoguanidine derivatives of loratadine. Bioorganic & medicinal chemistry letters. 2012 Oct 1;22(19):6076-80