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

Wukun Liu; Jinpei Zhou; Tong Zhang; Haiyang Zhu; Hai Qian; Huibin Zhang; Wenlong Huang; Ronald Gust

doi:10.1016/j.bmcl.2012.03.002

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. Epub 2012 Mar 8.

Authors

Wukun Liu¹, Jinpei Zhou, Tong Zhang, Haiyang Zhu, Hai Qian, Huibin Zhang, Wenlong Huang, Ronald Gust

Affiliation

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Anti-Inflammatory Agents / chemical synthesis*
Anti-Inflammatory Agents / chemistry
Anti-Inflammatory Agents / pharmacology
Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology
Biological Assay
Breast Neoplasms / drug therapy*
Cell Line, Tumor
Cell Proliferation / drug effects
Colonic Neoplasms / drug therapy*
Cyclization
Disease Models, Animal
Drug Design*
Female
Humans
Inhibitory Concentration 50
Mice
Pyrimidines / chemical synthesis*
Pyrimidines / chemistry
Pyrimidines / pharmacology
Thiourea / chemical synthesis*
Thiourea / chemistry
Thiourea / pharmacology

Substances

Anti-Inflammatory Agents
Antineoplastic Agents
Pyrimidines
Thiourea