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Esters of quinoxaline 1ˏ4-Di-N-oxide with cytotoxic activity on tumor cell lines based on NCI-60 panel
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نویسنده
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rivera g. ,shah s.s.a. ,arrieta-baez d. ,palos i. ,mongue a. ,sánchez-torres l.e.
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منبع
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iranian journal of pharmaceutical research - 2017 - دوره : 16 - شماره : 3 - صفحه:953 -965
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چکیده
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Quinoxalines display diverse and interesting pharmacological activities as antibacterial,antiviral,antiparasitic and anticancer agents. particularly,their 1ˏ4-di-n-oxide derivatives have proved to be cytotoxic agents that are active under hypoxic conditions as that of solid tumours. a new series of quinoxaline 1ˏ4-di-n-oxide substitutes at 7-position with esters group were synthetized and characterized by infrared (ir),proton nuclear magnetic resonance (1h-nmr),spectroscopy,and elemental analysis. seventeen derivatives (m1-m3,e1-e8,p1-p3 and dr1-dr3) were selected and evaluated for antitumor activities using the nci-60 human tumor cell lines screen. results showed that e7,p3 and e6 were the most active compounds against the cell lines tested. substitutions at 7-position with esters group not necessarily affect the biological activity,but the nature of the esters group could exert an influence on the selectivity. additionally,substitutions at 2-position influenced the cytotoxic activity of the compounds. © 2017 by school of pharmacy shaheed beheshti university of medical sciences and health services.
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کلیدواژه
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4-di-N-oxide; Antitumor; Cancer; Drugs; Esters; Quinoxaline 1
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آدرس
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centro de biotecnología genómica,instituto politécnico nacional,reynosa, Mexico, department of chemistry,quaid-i-azam university,islamabad, Pakistan, centro de nanociencias y micro y nanotecnología,instituto politécnico nacional,ciudad de méxico, Mexico, departamento de química aplicada,universidad autónoma de tamaulipas,reynosa, Mexico, neglected diseases section,drug r& d unit,center for applied pharmacobiology research,university of navarra,pamplona, Mexico, departamento de inmunología,escuela nacional de ciencias biológicas,instituto politécnico nacional,ciudad de méxico, Mexico
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Authors
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