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

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Title
A facile synthetic route to diazepinone derivatives via ring closing metathesis and its application for human cytidine deaminase inhibitors
Author(s)
M Kim; K Gajulapati; C Kim; H Y Jung; J Goo; K Lee; N Kaur; Hyo Jin Kang; Sang Jeon Chung; Y Choi
Bibliographic Citation
Chemical Communications, vol. 48, no. 93, pp. 11443-11445
Publication Year
2012
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
Publisher
Royal Soc Chem
DOI
http://dx.doi.org/10.1039/c2cc35484e
Type
Article
Appears in Collections:
1. Journal Articles > Journal Articles
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