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

被引：52

作者：

Liu, Wukun ^{[1
,2
]}

Zhou, Jinpei ^{[1
]}

Zhang, Tong ^{[1
]}

Zhu, Haiyang ^{[1
]}

Qian, Hai ^{[1
]}

Zhang, Huibin ^{[1
]}

Huang, Wenlong ^{[1
]}

Gust, Ronald ^{[2
,3
]}

机构：

[1] China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Peoples R China

[2] Free Univ Berlin, Inst Pharm, D-14195 Berlin, Germany

[3] Univ Innsbruck, Inst Pharm, A-6020 Innsbruck, Austria

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 08期

基金：

中国国家自然科学基金;

关键词：

Thioureas; Benzo[5,6]cyclohepta[1,2-b]pyridine; Antitumor; Anti-inflammation; ANTICANCER AGENTS; BIOLOGICAL EVALUATION; CELL-LINES; DESLORATADINE; ANTAGONISTS; DISCOVERY; HISTAMINE; ANALOGS; SERIES;

D O I：

10.1016/j.bmcl.2012.03.002

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：2701 / 2704

页数：4

共 29 条

[1] Anti-inflammatory properties of desloratadine [J].

Agrawal, DK .

CLINICAL AND EXPERIMENTAL ALLERGY, 2004, 34 (09) :1342-1348

[2] Synthesis, analgesic, anti-inflammatory, ulcerogenic index and antibacterial activities of novel 2-methylthio-3-substituted-5,6,7,8-tetrahydrobenzo(b)thieno[2,3-d]pyrimidin-4(3H)-ones [J].

Alagarsamy, V. ;

Meena, S. ;

Ramseshu, K. V. ;

Solomon, V. R. ;

Thirumurugan, K. ;

Dhanabal, K. ;

Murugan, M. .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2006, 41 (11) :1293-1300

[3] Checkpoint kinase 1-mediated phosphorylation of Cdc25C and bad proteins are involved in antitumor effects of loratadine-induced G2/M phase cell-cycle arrest and apoptosis [J].

Chen, Jinn-Shiun ;

Lin, Shyr-Yi ;

Tso, Wei-Ling ;

Yeh, Geng-Chang ;

Lee, Wen-Sen ;

Tseng, How ;

Chen, Li-Ching ;

Ho, Yuan-Soon .

MOLECULAR CARCINOGENESIS, 2006, 45 (07) :461-478

[4] Anti-inflammatory activity of H1-receptor antagonists:: review of recent experimental research [J].

Gelfand, EW ;

Appajosyula, S ;

Meeves, S .

CURRENT MEDICAL RESEARCH AND OPINION, 2004, 20 (01) :73-81

[5] A Series of α-Heterocyclic Carboxaldehyde Thiosemicarbazones Inhibit Topoisomerase IIα Catalytic Activity [J].

Huang, He ;

Chen, Qin ;

Ku, Xin ;

Meng, Linghua ;

Lin, Liping ;

Wang, Xiang ;

Zhu, Caihua ;

Wang, Yi ;

Chen, Zhi ;

Li, Ming ;

Jiang, Hualiang ;

Chen, Kaixian ;

Ding, Jian ;

Liu, Hong .

JOURNAL OF MEDICINAL CHEMISTRY, 2010, 53 (08) :3048-3064

[6] Synthesis, antiviral and anticancer activity of some novel thioureas derived from N-(4-nitro-2-phenoxyphenyl)-methanesulfonamide [J].

Karakus, Sevgi ;

Kucukguzel, S. Guniz ;

Kucukguzel, Ilkay ;

De Clercq, Erik ;

Pannecouque, Christophe ;

Andrei, Graciela ;

Snoeck, Robert ;

Sahin, Fikrettin ;

Bayrak, Oemer Faruk .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2009, 44 (09) :3591-3595

[7] Discovery of novel ureas and thioureas of 3-decladinosyl-3-hydroxy 15-membered azalides active against efflux-mediated resistant Streptococcus pneumoniae [J].

Krajacic, Mirjana Bukvic ;

Dumic, Miljenko ;

Novak, Predrag ;

Cindric, Mario ;

Kostrun, Sanja ;

Fajdetic, Andrea ;

Alihodzic, Sulejman ;

Brajsa, Karmen ;

Kujundzic, Nedjeljko .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2011, 21 (02) :853-856

[8] Synthesis and structure-activity relationships of N-benzyl-N-(X-2-hydroxybenzyl)-N′-phenylureas and thioureas as antitumor agents [J].

Li, Huan-Qiu ;

Yan, Tao ;

Yang, Ying ;

Shi, Lei ;

Zhou, Chang-Fang ;

Zhu, Hai-Liang .

BIOORGANIC & MEDICINAL CHEMISTRY, 2010, 18 (01) :305-313

[9] Urea Derivatives as Anticancer Agents [J].

Li, Huan-Qiu ;

Lv, Peng-Cheng ;

Yan, Tao ;

Zhu, Hai-Liang .

ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY, 2009, 9 (04) :471-480

[10] Design, synthesis and antitumor evaluation of a new series of N-substituted-thiourea derivatives [J].

Li, Jian ;

Tan, Jin-zhi ;

Chen, Li-li ;

Zhang, Jian ;

Shen, Xu ;

Mei, Chang-lin ;

Fu, Li-li ;

Lin, Li-ping ;

Ding, Jian ;

Xiong, Bing ;

Xiong, Xi-shan ;

Liu, Hong ;

Luo, Xiao-min ;

Jiang, Hua-liang .

ACTA PHARMACOLOGICA SINICA, 2006, 27 (09) :1259-1271

← 1 2 3 →