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Title 

A facile synthetic route to diazepinone derivatives via ring closing metathesis and its application for human cytidine deaminase inhibitors

Authors 

M KimK GajulapatiC KimH Y JungJ GooK LeeN KaurHyo Jin KangSang Jeon ChungY Choi

Publisher 

Royal Society of Chemistry

Issue Date 

2012

Citation 

Chemical Communications, vol. 48, no. 93, pp. 11443-11445

Abstract 

A variety of diazepinone derivatives were prepared from α-amino acids and amino alcohols by a new synthetic methodology based on ring closing metathesis as a key step. The diazepinones were coupled with ribose derivatives to afford novel diazepinone nucleosides. Among them, (4R)-1-ribosyl-4-methyl-3, 4-dihydro-1H-1,3-diazepin-2(7H)-one (3) showed a potent inhibitory effect (K i = 145.97 ± 4.87 nM) against human cytidine deaminase.

ISSN 

1359-7345

Link 

http://dx.doi.org/10.1039/c2cc35484e

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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