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Synthesis and in vitro anticancer activity of 6,7-methylenedioxy (or 5-hydroxy-6-methoxy)-2-(substituted selenophenyl)quinolin-4-one analogs
- Source :
- European Journal of Medicinal Chemistry. 46:6046-6056
- Publication Year :
- 2011
- Publisher :
- Elsevier BV, 2011.
-
Abstract
- 6,7-Methylenedioxy (or 5-hydroxy-6-methoxy)-2-(substituted selenophenyl)quinolin-4-ones and their isosteric compounds were synthesized and evaluated for anticancer activity. Structure–activity relationships (SAR) of these compounds were established. Among all tested compounds, 6,7-methylenedioxy-2-(5-methylselenophen-2-yl)quinolin-4-one (4d) was found to be the most promising anticancer agent. In screening against NCI’s 60 human tumor cell line panel, 4d exhibited highly selective and potent inhibitory activity against MDA-MB-435 melanoma. Furthermore, the results of COMPARE analysis suggested that 4d is an antimitotic agent with a different mechanism of action from the conventional antimitotic agents, such as colchicine, vinca alkaloids and paclitaxel. Therefore, 4d was identified as a new lead compound that merits further optimization.
- Subjects :
- Vinca
Stereochemistry
Antineoplastic Agents
Methylenedioxy
Structure-Activity Relationship
chemistry.chemical_compound
Cell Line, Tumor
Neoplasms
Organoselenium Compounds
Drug Discovery
Benzene Derivatives
medicine
Humans
Cell Proliferation
Pharmacology
biology
Organic Chemistry
General Medicine
biology.organism_classification
Combinatorial chemistry
In vitro
Paclitaxel
chemistry
Mechanism of action
Cell culture
Quinolines
Antimitotic Agent
Drug Screening Assays, Antitumor
medicine.symptom
Lead compound
Subjects
Details
- ISSN :
- 02235234
- Volume :
- 46
- Database :
- OpenAIRE
- Journal :
- European Journal of Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....e8ffc7008d373ad69a808e87c260254b