Thienopyridine and Benzofuran Derivatives as Potent Antitumor Agents Possessing Different Structure—Activity Relationships
| Autor: | Rieko Shioya, Hidehiko Furukawa, Yuichi Sugano, Toshinori Agatsuma, Ichiro Hayakawa |
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| Rok vydání: | 2004 |
| Předmět: |
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 |
| Zdroj: | ChemInform. 35 |
| ISSN: | 1522-2667 0931-7597 |
| Popis: | (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. |
| Databáze: | OpenAIRE |
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