Department of Medicinal Chemistry, China Pharmaceutical University, Tongjia Xiang 24, Nanjing, PR China.
Bioorg Med Chem Lett. 2012 Apr 15;22(8):2701-4. doi: 10.1016/j.bmcl.2012.03.002. Epub 2012 Mar 8.
Thiourea derivatives (6a-e) were developed and screened for antitumor and anti-inflammatory activity. Most of the compounds exhibited growth inhibitory effects comparable to 5-fluorouracil in vitro against mammary (MCF-7 and MDA-MB 231) as well as colon (HT-29) carcinoma cells. They also showed stronger anti-inflammatory activity than ibuprofen in vivo in the xylene-induced ear swelling assay in mice.
硫脲衍生物(6a-e)被开发并筛选用于抗肿瘤和抗炎活性。大多数化合物在体外对乳腺癌(MCF-7 和 MDA-MB 231)和结肠癌(HT-29)细胞表现出与 5-氟尿嘧啶相当的生长抑制作用。它们在体内也显示出比布洛芬更强的抗炎活性,在二甲苯诱导的小鼠耳肿胀试验中。