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含苯并[5,6]环庚[1,2-b]吡啶部分的硫脲衍生物的设计与合成作为潜在的抗肿瘤和抗炎药物。

Design and synthesis of thiourea derivatives containing a benzo[5,6]cyclohepta[1,2-b]pyridine moiety as potential antitumor and anti-inflammatory agents.

机构信息

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

出版信息

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2701-4. doi: 10.1016/j.bmcl.2012.03.002. Epub 2012 Mar 8.

DOI:10.1016/j.bmcl.2012.03.002
PMID:22450132
Abstract

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.

摘要

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。

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