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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
- Files in This Item:
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