|
rdf:type |
|
|
lifeskim:mentions |
umls-concept:C0007097,
umls-concept:C0038477,
umls-concept:C0205314,
umls-concept:C0205369,
umls-concept:C0205460,
umls-concept:C0220781,
umls-concept:C0220825,
umls-concept:C0439611,
umls-concept:C0450442,
umls-concept:C0679622,
umls-concept:C1533691,
umls-concept:C1883254,
umls-concept:C2239176,
umls-concept:C2936588
|
|
pubmed:issue |
21
|
|
pubmed:dateCreated |
2010-10-11
|
|
pubmed:abstractText |
Novel thienopyridine derivatives 1b-1r were synthesized, based on a hit compound 1a that was found in a previous cell-based screening of anticancer drugs. Compounds 1a-1r have the following features: (1) their anticancer activity in vitro was first reported by our group. (2) The most potent analog 1g possesses hepatocellular carcinoma (HCC)-specific anticancer activity. It can specifically inhibit the proliferation of the human hepatoma HepG2 cells with an IC(50) value of 0.016?M (compared with doxorubicin as a positive control, whose IC(50) was 0.37?M). It is inactive toward a panel of five different types of human cancer cell lines. (3) Compound 1g remarkably induces G(0)/G(1) arrest and apoptosis in HepG2 cells in vitro at low micromolar concentrations. These results, especially the HCC-specific anticancer activity of 1g, suggest their potential in targeted chemotherapy for HCC.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Nov
|
|
pubmed:issn |
1464-3405
|
|
pubmed:author |
pubmed-author:HeHai-YunHY,
pubmed-author:LiuJi-YanJY,
pubmed-author:SongXiang-RongXR,
pubmed-author:TongAi-PingAP,
pubmed-author:WeiYu-QuanYQ,
pubmed-author:XiangMing-LiML,
pubmed-author:YangLiL,
pubmed-author:YangSheng-YongSY,
pubmed-author:YuLuo-TingLT,
pubmed-author:ZengXiu-XiuXX,
pubmed-author:ZhaoYing-LanYL,
pubmed-author:ZhengRen-LinRL,
pubmed-author:ZhengYuY,
pubmed-author:ZhouTianT
|
|
pubmed:copyrightInfo |
Copyright © 2010 Elsevier Ltd. All rights reserved.
|
|
pubmed:issnType |
Electronic
|
|
pubmed:day |
1
|
|
pubmed:volume |
20
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
6282-5
|
|
pubmed:meshHeading |
pubmed-meshheading:20846862-Antibiotics, Antineoplastic,
pubmed-meshheading:20846862-Antineoplastic Agents,
pubmed-meshheading:20846862-Apoptosis,
pubmed-meshheading:20846862-Carcinoma, Hepatocellular,
pubmed-meshheading:20846862-Cell Line, Tumor,
pubmed-meshheading:20846862-Cell Proliferation,
pubmed-meshheading:20846862-Cyclization,
pubmed-meshheading:20846862-DNA,
pubmed-meshheading:20846862-Doxorubicin,
pubmed-meshheading:20846862-Flow Cytometry,
pubmed-meshheading:20846862-G0 Phase,
pubmed-meshheading:20846862-G1 Phase,
pubmed-meshheading:20846862-Humans,
pubmed-meshheading:20846862-Liver Neoplasms,
pubmed-meshheading:20846862-Magnetic Resonance Spectroscopy,
pubmed-meshheading:20846862-Spectrometry, Mass, Electrospray Ionization,
pubmed-meshheading:20846862-Structure-Activity Relationship,
pubmed-meshheading:20846862-Thienopyridines
|
|
pubmed:year |
2010
|
|
pubmed:articleTitle |
Novel thienopyridine derivatives as specific anti-hepatocellular carcinoma (HCC) agents: synthesis, preliminary structure-activity relationships, and in vitro biological evaluation.
|
|
pubmed:affiliation |
State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medicinal School, Sichuan University, Chengdu 610041, Sichuan, China.
|
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|
