Abstract
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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Benzamides / chemistry*
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Benzamides / isolation & purification
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Benzamides / pharmacology
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Biocatalysis
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Caspase 3 / metabolism
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Caspase Inhibitors
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Crystallography, X-Ray
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Magnetic Resonance Spectroscopy
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Molecular Conformation
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Quinazolines / chemistry*
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Quinazolines / isolation & purification
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Quinazolines / pharmacology
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Streptomyces / chemistry*
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ortho-Aminobenzoates / chemistry*
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ortho-Aminobenzoates / isolation & purification
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ortho-Aminobenzoates / pharmacology
Substances
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3-hydroxyl-2-N-iso-butyryl-anthranilamide
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Benzamides
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Caspase Inhibitors
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Quinazolines
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ortho-Aminobenzoates
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Caspase 3