期刊
CHEMICAL & PHARMACEUTICAL BULLETIN
卷 59, 期 4, 页码 447-451出版社
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.59.447
关键词
Streptomyces sp.; benzamide; quinazoline; Caspase-3
资金
- National Natural Science Foundation of China [U0633008]
- Ministry of Science and Technology of China [2009CB522300, 2008ZX09401-05, 2009ZX09302-004]
- Ministry of Education of China/Fok Ying Tung Education Foundation [121039]
- State Key Laboratory of Drug Rearch [SIMM0812KF-02]
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 IC50 values of 32 and 36 mu M, respectively.
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