Phenyl-substituted dihydropyrazines with DNA strand-breakage activity.

نویسندگان

  • Shigeru Ito
  • Shinji Takechi
  • Kazuhide Nakahara
  • Nobuhiro Kashige
  • Tadatoshi Yamaguchi
چکیده

Monophenyl-substituted dihydropyrazines (Ph-DHP-1 to 4) of 2,3-dihydro-5,6-dimethylpyrazine (Me-DHP-1), which have the inductive effects of apoptosis and mutagenesis, were synthesized and their biological effect was investigated in terms of DNA strand-breakage. Differences between the phenyl- and methyl-substituted dihydropyrazines were examined.

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منابع مشابه

Biol. Pharm. Bull. 30(9) 1663—1667 (2007)

of dihydropyrazines (DHPs) such as 2,3-dihydro-5,6-dimethylpyrazine (Me-DHP), which causes DNA strand breakage in the plasmid pBR322. We showed that DHPs inhibit growth and cause mutagenesis in Escherichia coli and that Me-DHP is cytotoxic and genotoxic in E. coli due to the production of radical species in the presence of Cu . Phenyl substituted dihydropyrazines (Ph-DHPs) have much higher DNA ...

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Radical species in DNA strand-cleavage caused by dihydropyrazines.

Dihydropyrazines (DHPs), which generate hydroxyl and carbon-centered radicals, cleaved DNA single-strand. It is new knowledge that DHPs were recently determined to produce 8-hydroxydeoxyguanosine. The remarkable increase in the DNA strand-cleavage activity upon the addition of Cu2+ suggests that the primary reactive species is carbon-centered radicals rather than the hydroxyl radical generated ...

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Synthesis and Antimicrobial Activity of Some 2-[(4-Substituted-Phenyl-3-Chloro-Azetidin-2-One)-5-(2'-Methylamino-4-Phenyl-1', 3'-Thiazolyl-]-1, 3,4-Thiadiazoles

A new 2-[(4-substituted-phenyl-3-chloroazetidin-2-one)-5-(2'-methylamino 4-phenyl-1', 3'-thiazolyl-]-1, 3, 4-thiadiazoles, 5(a-n) were synthesized from 2-substituted-benzylideneamino-5-[2'-methylamino-4'-phenyl-1',3'-thiazolyl]-1,3, 4-thiadiazole, 4(a-n) using 2-amino-4phenyl-1, 3-thiazole as a starting material. The synthesised compounds have been screened in vitro for their antimicrobial acti...

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عنوان ژورنال:
  • Chemical & pharmaceutical bulletin

دوره 58 6  شماره 

صفحات  -

تاریخ انتشار 2010