Benzamides and Quinazolines from a Mangrove Actinomycetes Streptomyces sp. (No. 061316) and Their Inhibiting Caspase-3 Catalytic Activity in Vitro
| Autor: | Guo-Dong Chen, Huinan Zhao, Qing-Yi Xie, Jia Li, Kui Hong, Xin-Sheng Yao, Hai-Peng Lin, Yuan-Fan Huang, Jin-Shan Tang, Hao Gao, Ying Chen, Ying Wang |
|---|---|
| Rok vydání: | 2011 |
| Předmět: |
Magnetic Resonance Spectroscopy
Stereochemistry Electrospray ionization Molecular Conformation Caspase 3 Crystallography X-Ray Streptomyces chemistry.chemical_compound Drug Discovery Quinazoline ortho-Aminobenzoates Benzamide biology General Chemistry General Medicine Nuclear magnetic resonance spectroscopy biology.organism_classification Caspase Inhibitors In vitro chemistry Biocatalysis Benzamides Quinazolines |
| Zdroj: | Chemical and Pharmaceutical Bulletin. 59:447-451 |
| ISSN: | 1347-5223 0009-2363 |
| DOI: | 10.1248/cpb.59.447 |
| Popis: | One new benzamide, 3-hydroxyl-2-N-iso-butyryl-anthranilamide (1), together with two known benzamides (2, 3) and three known quinazolines (4-6), was isolated from a mangrove actinomycetes Streptomyces sp. (No. 061316), which displayed inhibiting Caspase-3 activity in vitro. The structure of 1 was elucidated by electrospray ionization (ESI)-MS, NMR spectroscopies and X-ray crystal diffraction. After evaluation of all compounds for their inhibitory effect on Caspase-3 in vitro, 3-hydroxyl-anthranilamide (2) and 8-hydroxyl-2,4-dioxoquinazoline (6) showed activity against Caspase-3 with IC(50) values of 32 and 36 µM, respectively. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|