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Thienopyridine and Benzofuran Derivatives as Potent Antitumor Agents Possessing Different Structure—Activity Relationships
- Source :
- ChemInform. 35
- Publication Year :
- 2004
- Publisher :
- Wiley, 2004.
-
Abstract
- (3-Amino-6-thiophen-2-yl-thieno[2,3-b]pyridin-2-yl)phenylmethanone (3) was discovered as a new type of cytotoxic agent selective against a tumorigenic cell line. The molecular structure of a previously reported compound, (4-hydroxy-3-methyl-6-phenylbenzofuran-2-yl)phenylmethanone (2), had remarkably similar bioisosteric substructures to that of compound 3. Although the relationship between the molecular structure and biological activity of each derivative synthesized from these two hit compounds (2 and 3) were studied, unexpectedly no correlation was observed. However, after further synthetic study from 3, one of the most potent derivative (10k) having a different SAR profile from 2, was discovered.
- Subjects :
- Thienopyridine
Pyridines
Stereochemistry
Clinical Biochemistry
Pharmaceutical Science
Antineoplastic Agents
Biochemistry
Chemical synthesis
Inhibitory Concentration 50
Structure-Activity Relationship
chemistry.chemical_compound
Cell Line, Tumor
Drug Discovery
Humans
Structure–activity relationship
Benzofuran
Molecular Biology
Benzofurans
Bicyclic molecule
Organic Chemistry
Biological activity
General Medicine
chemistry
Molecular Medicine
Bioisostere
Lead compound
Subjects
Details
- ISSN :
- 15222667 and 09317597
- Volume :
- 35
- Database :
- OpenAIRE
- Journal :
- ChemInform
- Accession number :
- edsair.doi.dedup.....40930ada9dd102540a4e50a21a8781b3