Source:http://linkedlifedata.com/resource/pubmed/id/19221468
Switch to
| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
5
|
| pubmed:dateCreated |
2009-5-6
|
| pubmed:abstractText |
Previously, we discovered a novel class of salicylhydrazide compounds with remarkable activity in hormone-dependent and -independent human cancer cells. We then designed and synthesized numerous analogues. Among these analogues, a quinoxalinhydrazide compound, SC144, exhibited desirable physicochemical and drug-like properties and therefore was selected for further preclinical investigation. In the present study, we evaluated the in vitro activity of SC144 in a range of drug-sensitive and -resistant cancer cell lines as well as its in vivo efficacy in MDA-MB-435 and HT29 mice xenograft models. The broad-spectrum cytotoxicity of SC144 is especially highlighted by its potency in ovarian cancer cells resistant to cisplatin, breast-cancer cells resistant to doxorubicin, and colon cancer cells resistant to oxaliplatin. Furthermore, its activity was independent of p53, HER-2, estrogen and androgen receptor expressions. We also examined the effect of SC144 on cell cycle progression and apoptosis in select cell lines. Considering its cytotoxicity profile in a variety of in vitro and in vivo cancer models as well as its effects on cell cycle regulation and apoptosis, SC144 appears to represent a promising agent for further clinical development.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Mar
|
| pubmed:issn |
1555-8576
|
| pubmed:author | |
| pubmed:issnType |
Electronic
|
| pubmed:volume |
8
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
458-65
|
| pubmed:meshHeading |
pubmed-meshheading:19221468-Animals,
pubmed-meshheading:19221468-Antineoplastic Agents,
pubmed-meshheading:19221468-Cell Cycle,
pubmed-meshheading:19221468-Cell Line, Tumor,
pubmed-meshheading:19221468-Cell Survival,
pubmed-meshheading:19221468-Cytochrome P-450 Enzyme System,
pubmed-meshheading:19221468-Dose-Response Relationship, Drug,
pubmed-meshheading:19221468-Drug Discovery,
pubmed-meshheading:19221468-Female,
pubmed-meshheading:19221468-Flow Cytometry,
pubmed-meshheading:19221468-HT29 Cells,
pubmed-meshheading:19221468-Humans,
pubmed-meshheading:19221468-Hydrazines,
pubmed-meshheading:19221468-Inhibitory Concentration 50,
pubmed-meshheading:19221468-Mice,
pubmed-meshheading:19221468-Mice, Nude,
pubmed-meshheading:19221468-Molecular Structure,
pubmed-meshheading:19221468-Neoplasms,
pubmed-meshheading:19221468-Quinoxalines,
pubmed-meshheading:19221468-Xenograft Model Antitumor Assays
|
| pubmed:year |
2009
|
| pubmed:articleTitle |
Discovery of a novel quinoxalinhydrazide with a broad-spectrum anticancer activity.
|
| pubmed:affiliation |
Department of Pharmacology and Pharmaceutical Sciences, School of Pharmacy, University of Southern California, Los Angeles, California 90033, USA.
|
| pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, Non-P.H.S.,
Research Support, Non-U.S. Gov't
|