A facile synthetic route to diazepinone derivatives via ring closing metathesis and its application for human cytidine deaminase inhibitors
M Kim, K Gajulapati, C Kim, HY Jung, J Goo…
Index: Kim, Minkyoung; Gajulapati, Kondaji; Kim, Chorong; Jung, Hwa Young; Goo, Jail; Lee, Kyeong; Kaur, Navneet; Kang, Hyo Jin; Chung, Sang J.; Choi, Yongseok Chemical Communications, 2012 , vol. 48, # 93 p. 11443 - 11445
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Citation Number: 4
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 (Ki= 145.97±4.87 nM) against human cytidine deaminase.
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