|
rdf:type |
|
|
lifeskim:mentions |
umls-concept:C0005532,
umls-concept:C0205224,
umls-concept:C0205460,
umls-concept:C0220806,
umls-concept:C0392747,
umls-concept:C0441655,
umls-concept:C0599740,
umls-concept:C0630889,
umls-concept:C0680730,
umls-concept:C1148554,
umls-concept:C1554963,
umls-concept:C1566558,
umls-concept:C2603343
|
|
pubmed:issue |
4
|
|
pubmed:dateCreated |
2011-3-4
|
|
pubmed:abstractText |
Caged 4-oxa-tricyclo[4.3.1.0(3,7)]dec-2-one structural motifs are found in Garcinia natural products that demonstrate anti-tumor activity. Gambogic acid (GA, 1), the most abundant caged Garcinia xanthones, has been reported to be a promising anti-cancer agent. To identify the essential pharmacophore for its anti-tumor activity, a series of GA analogues that address potential key structural features for biological activity were synthesized, among which compound 11a displayed comparable in vitro anti-tumor activity as GA. Mechanistic studies on 11a determined that the compound induces apoptosis as well as arrests the G2/M phase of the cell cycle in HepG2 cells. The determination of the essential part of the scaffold found in GA to maintain anti-tumor effects, and the SAR based on the caged pharmacophore are reported and will provide key information for future anti-cancer drug development studies.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Apr
|
|
pubmed:issn |
1768-3254
|
|
pubmed:author |
pubmed-author:GaoYuanY,
pubmed-author:GongDandanD,
pubmed-author:GuoQinglongQ,
pubmed-author:LinChangjunC,
pubmed-author:PaiR PRP,
pubmed-author:WangXiaojianX,
pubmed-author:WeiLibingL,
pubmed-author:XiMeiyangM,
pubmed-author:YangQianQ,
pubmed-author:YouQidongQ,
pubmed-author:ZhangShenglieS
|
|
pubmed:copyrightInfo |
Copyright © 2011 Elsevier Masson SAS. All rights reserved.
|
|
pubmed:issnType |
Electronic
|
|
pubmed:volume |
46
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
1280-90
|
|
pubmed:dateRevised |
2011-11-17
|
|
pubmed:meshHeading |
pubmed-meshheading:21334116-Animals,
pubmed-meshheading:21334116-Antineoplastic Agents,
pubmed-meshheading:21334116-Apoptosis,
pubmed-meshheading:21334116-Biological Agents,
pubmed-meshheading:21334116-Carcinoma, Hepatocellular,
pubmed-meshheading:21334116-Caspase 3,
pubmed-meshheading:21334116-Cell Cycle,
pubmed-meshheading:21334116-Cell Line, Tumor,
pubmed-meshheading:21334116-Cell Proliferation,
pubmed-meshheading:21334116-Gene Expression Regulation, Neoplastic,
pubmed-meshheading:21334116-Humans,
pubmed-meshheading:21334116-Mice,
pubmed-meshheading:21334116-Proto-Oncogene Proteins c-bcl-2,
pubmed-meshheading:21334116-Structure-Activity Relationship,
pubmed-meshheading:21334116-Xanthones,
pubmed-meshheading:21334116-Xenograft Model Antitumor Assays,
pubmed-meshheading:21334116-bcl-2-Associated X Protein
|
|
pubmed:year |
2011
|
|
pubmed:articleTitle |
Studies on chemical modification and biology of a natural product, gambogic acid (III): determination of the essential pharmacophore for biological activity.
|
|
pubmed:affiliation |
Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
|
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|
