Synthesis and in vitro antiproliferative activity of C5-benzyl substituted 2-amino-pyrrolo[2,3-d]pyrimidines as potent Hsp90 inhibitors
- Authors
- Lee, Ju-Hyeon; Shin, Sang Chul; Seo, Seon Hee; Seo, Young Ho; Jeong, Nakcheol; Kim, Chan-Wha; Kim, Eunice EunKyeong; Keum, Gyochang
- Issue Date
- 15-1월-2017
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Hsp90; Structure-based design; Cancer; Antiproliferative; Pyrrolo[2,3-d]pyrimidines
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.27, no.2, pp.237 - 241
- Indexed
- SCIE
SCOPUS
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 27
- Number
- 2
- Start Page
- 237
- End Page
- 241
- URI
- https://scholar.korea.ac.kr/handle/2021.sw.korea/84909
- DOI
- 10.1016/j.bmcl.2016.11.062
- ISSN
- 0960-894X
- Abstract
- A novel series of heat shock protein 90 (Hsp90) inhibitors was identified by X-ray crystal analysis of complex structures at solvent-exposed exit pocket C. The 2-amino-pyrrolo[2,3-d]pyrimidine derivatives, 7-deazapurines substituted with a benzyl moiety at C5, showed potent Hsp90 inhibition and broadspectrum antiproliferative activity against NCI-60 cancer cell lines. The most potent compound, 6a, inhibited Hsp90 with an IC50 of 36 nM and showed a submicromolar mean GI(50) value against NCI-60 cell lines. The interaction of 6a at the ATP-binding pocket of Hsp90 was confirmed by X-ray crystallography and Western blot analysis. (C) 2016 Published by Elsevier Ltd.
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Collections - College of Science > Department of Chemistry > 1. Journal Articles
- College of Life Sciences and Biotechnology > Division of Life Sciences > 1. Journal Articles
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