title: Benzamides and quinazolines from a mangrove actinomycetes Streptomyces sp. (No. 061316) and their inhibiting caspase-3 catalytic activity in vitro.
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.
authors.affiliation: Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy/Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, Jinan University, Guangzhou, People’s Republic of China.
authors.forename: Guodong
authors.initials: G
authors.lastname: Chen
authors.forename: Hao
authors.initials: H
authors.lastname: Gao
authors.forename: Jinshan
authors.initials: J
authors.lastname: Tang
authors.forename: Yuanfan
authors.initials: Y
authors.lastname: Huang
authors.forename: Ying
authors.initials: Y
authors.lastname: Chen
authors.forename: Ying
authors.initials: Y
authors.lastname: Wang
authors.forename: Huinan
authors.initials: H
authors.lastname: Zhao
authors.forename: Haipeng
authors.initials: H
authors.lastname: Lin
authors.forename: Qingyi
authors.initials: Q
authors.lastname: Xie
authors.forename: Kui
authors.initials: K
authors.lastname: Hong
authors.forename: Jia
authors.initials: J
authors.lastname: Li
authors.forename: Xinsheng
authors.initials: X
authors.lastname: Yao
mesh_terms: D001549:Benzamides / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D055162:Biocatalysis; D053148:Caspase 3 / Q000378:metabolism; D061945:Caspase Inhibitors; D018360:Crystallography, X-Ray; D009682:Magnetic Resonance Spectroscopy; D008968:Molecular Conformation; D011799:Quinazolines / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D013302:Streptomyces / Q000737:chemistry*; D062367:ortho-Aminobenzoates / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology
chemical_list: C559410:3-hydroxyl-2-N-iso-butyryl-anthranilamide; D001549:Benzamides; D061945:Caspase Inhibitors; D011799:Quinazolines; D062367:ortho-Aminobenzoates; D053148:Caspase 3