4.3 Article

Benzamides and Quinazolines from a Mangrove Actinomycetes Streptomyces sp (No. 061316) and Their Inhibiting Caspase-3 Catalytic Activity in Vitro

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

  1. National Natural Science Foundation of China [U0633008]
  2. Ministry of Science and Technology of China [2009CB522300, 2008ZX09401-05, 2009ZX09302-004]
  3. Ministry of Education of China/Fok Ying Tung Education Foundation [121039]
  4. State Key Laboratory of Drug Rearch [SIMM0812KF-02]

向作者/读者索取更多资源

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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