1. Academic Validation
  2. Synthesis and biological evaluation of cyanoguanidine derivatives of loratadine

Synthesis and biological evaluation of cyanoguanidine derivatives of loratadine

  • Bioorg Med Chem Lett. 2012 Oct 1;22(19):6076-80. doi: 10.1016/j.bmcl.2012.08.041.
Wukun Liu 1 Jinpei Zhou Tong Zhang Huibin Zhang Haiyang Zhu Yanhua Cheng Ronald Gust
Affiliations

Affiliation

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

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.

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