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A facile synthetic route to diazepinone derivatives via ring closing metathesis and its application for human cytidine deaminase inhibitors
- Kim, Minkyoung;
- Gajulapati, Kondaji;
- Kim, Chorong;
- Jung, Hwa Young;
- Goo, Jail;
- ... Choi, Yongseok;
- 외 4명
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15초록
A variety of diazepinone derivatives were prepared from alpha-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-1 = 145.97 +/- 4.87 nM) against human cytidine deaminase.
키워드
CYCLIC UREA NUCLEOSIDES; CYTOSINE-ARABINOSIDE; CARBOCYCLIC ANALOGS; POTENT; 5-AZA-2'-DEOXYCYTIDINE; ZEBULARINE; RESISTANCE; RIBOSIDE; AFFINITY; BINDING
- 제목
- A facile synthetic route to diazepinone derivatives via ring closing metathesis and its application for human cytidine deaminase inhibitors
- 저자
- Kim, Minkyoung; Gajulapati, Kondaji; Kim, Chorong; Jung, Hwa Young; Goo, Jail; Lee, Kyeong; Kaur, Navneet; Kang, Hyo Jin; Chung, Sang J.; Choi, Yongseok
- 발행일
- 2012
- 유형
- Article
- 권
- 48
- 호
- 93
- 페이지
- 11443 ~ 11445