Acta Pharmaceutica, Vol. 60 No. 1, 2010.
Izvorni znanstveni članak
https://doi.org/10.2478/v10007-010-0004-0
Synthesis and biological activity of some new 1-benzyl and 1-benzoyl 3-heterocyclic indole derivatives
ESLAM REDA EL-SAWY
; Chemistry Department of Natural Compounds, National Research Centre, Cairo, Egypt
FATMA A. BASSYOUNI
; Chemistry Department of Natural and Microbial Products, National Research Centre, Cairo, Egypt
SHERIFA H. ABU-BAKR
; Chemistry Department of Natural and Microbial Products, National Research Centre, Cairo, Egypt
HANAA M. RADY
; Chemistry Department of Natural Compounds, National Research Centre, Cairo, Egypt
MOHAMED M. ABDLLA
; Univeterinary Research Unit, Pharmaceutical Company, Cairo, Egypt
Sažetak
Starting from 1-benzyl- (2a) and 1-benzoyl-3-bromoacetyl indoles (2b) new heterocyclic, 2-thioxoimidazolidine (4a,b), imidazolidine-2,4-dione (5a,b), pyrano(2,3-d)imidazole (8a,b and 9a,b), 2-substituted quinoxaline (11a,b–17a,b) and triazolo(4,3-a)quinoxaline derivatives (18a,b and 19a,b) were synthesized and evaluated for their antimicrobial and anticancer activities. Antimicrobial activity screening performed with concentrations of 0.88, 0.44 and 0.22 g mm2 showed that 3-(1-substituted indol-3-yl)quinoxalin-2(1H)ones (11a,b) and 2-(4-methyl piperazin-1-yl)-3-(1-substituted indol-3-yl) quinoxalines (15a,b) were the most active of all the tested compounds towards P. aeruginosa, B. cereus and S. aureus compared to the reference drugs cefotaxime and piperacillin, while 2-chloro-3-(1-substituted indol-3-yl)quinoxalines (12a,b) were the most active against C. albicans compared to the reference drug nystatin. On the other hand, 2-chloro-3-(1-benzyl indol-3-yl) quinoxaline (12a) display potent efficacy against ovarian cancer xenografts in nude mice with tumor growth suppression of 100 0.3 %.
Ključne riječi
2-chloro-3-(1-benzyl)quinoxalines; 2-chloro-3-(1-benzoylindol-3-yl)quinoxalines; antimicrobial; ovarian anti-cancer
Hrčak ID:
48278
URI
Datum izdavanja:
1.3.2010.
Posjeta: 3.161 *