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Asymmetric Synthesis of Fluoro-MLN4924 as a Selective NEDD8-Activating Enzyme (NAE) Inhibitor
- Kim, Hong-Rae;
- Jarhad, Dnyandev B.;
- Sahu, Pramod K.;
- Sung, Kisu;
- An, Dayoung;
- 외 3명
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2초록
Based on bioisosteric rationale, fluorinated analogues of MLN4924, which is a selective NEDD8-activating enzyme inhibitor, were designed and their asymmetric syntheses were accomplished via stereoselective reduction, regioselective isopropylidene cleavage and diethylaminosulfur trifluoride (DAST) fluorination as key steps.
키워드
MLN4924; Fluoro-MLN4924; Bioisotere; NEDD8 inhibitor; DAST fluorination; PEVONEDISTAT TAK-924/MLN4924; STEREOSELECTIVE-SYNTHESIS; PROTEIN-DEGRADATION; DRUG DISCOVERY; HUMAN-DISEASES; PHASE-I; UBIQUITIN; NUCLEOSIDES; BORTEZOMIB; MLN4924
- 제목
- Asymmetric Synthesis of Fluoro-MLN4924 as a Selective NEDD8-Activating Enzyme (NAE) Inhibitor
- 저자
- Kim, Hong-Rae; Jarhad, Dnyandev B.; Sahu, Pramod K.; Sung, Kisu; An, Dayoung; Hyun, Young Eum; Yu, Jinha; Jeong, Lak Shin
- 발행일
- 2019-09
- 유형
- Article
- 권
- 8
- 호
- 9
- 페이지
- 1641 ~ 1647
- 언어
- ENG
- 출판사
- Wiley - VCH Verlag GmbH & Co. KG
- 발행국가
- 독일
- 분량
- 7 페이지
- ISSN
- E 2193-5815
P 2193-5807