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

  • Bioorg Med Chem Lett. 2012 Apr 15;22(8):2701-4. doi: 10.1016/j.bmcl.2012.03.002.
Wukun Liu  1 ,  Jinpei Zhou ,  Tong Zhang ,  Haiyang Zhu ,  Hai Qian ,  Huibin Zhang ,  Wenlong Huang ,  Ronald Gust
Affiliations
  • 1. Department of Medicinal Chemistry, China Pharmaceutical University, Tongjia Xiang 24, Nanjing, PR China.
PMID: 22450132 DOI: 10.1016/j.bmcl.2012.03.002
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.