Synthesis and biological evaluation of cyanoguanidine derivatives of loratadine |
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| Authors: | Wukun Liu Jinpei Zhou Tong Zhang Huibin Zhang Haiyang Zhu Yanhua Cheng Ronald Gust |
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| Institution: | 1. Department of Medicinal Chemistry, China Pharmaceutical University, Tongjia Xiang 24, 210009 Nanjing, PR China;2. Institute of Pharmacy, Freie Universität Berlin, Königin-Luise-Str, 2+4, 14195 Berlin, Germany;3. Institute of Pharmacy, University of Innsbruck, Innrain 80/82, A-6020 Innsbruck, Austria |
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| Abstract: | Cyanoguanidine derivatives of loratadine (3a–i) were synthesized and screened for antitumor and anti-inflammatory activity. The most promising compound 3c (R = n-C8H17) 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. |
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