Department of Medicinal Chemistry, China Pharmaceutical University, Tongjia Xiang 24, 210009 Nanjing, PR China.
Bioorg Med Chem Lett. 2012 Oct 1;22(19):6076-80. doi: 10.1016/j.bmcl.2012.08.041. Epub 2012 Aug 16.
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.
氯雷他定的氰胍衍生物（3a-i）被合成并进行了抗肿瘤和抗炎活性筛选。最有前途的化合物 3c（R=n-C（8）H（17））在体外对乳腺癌（MCF-7 和 MDA-MB 231）和结肠癌（HT-29）细胞的细胞毒性至少比 5-氟尿嘧啶高两倍。然而，其作用模式目前尚不清楚。细胞毒性作用不太可能涉及 COX-1/2 酶。然而，所有化合物在二甲苯诱导的小鼠耳肿胀试验中均显示出比布洛芬更强的体内抗炎活性。
