Synthetic strategy for increasing solubility of potential FLT3 inhibitor thieno[2,3-d]pyrimidine derivatives through structural modifications at the C-2 and C-6 positions
- Authors
- Oh, Changmok; Kim, Hyuntae; Kang, Jong Soon; Yun, Jieun; Sim, Jaejun; Kim, Hwan-Mook; Han, Gyoonhee
- Issue Date
- 1-Feb-2017
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- FLT3; Thieno[2,3-d]pyrimidine; Acute myeloid leukemia (AML); Solubility
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.27, no.3, pp.496 - 500
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 27
- Number
- 3
- Start Page
- 496
- End Page
- 500
- URI
- https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/6403
- DOI
- 10.1016/j.bmcl.2016.12.034
- ISSN
- 0960-894X
- Abstract
- Acute myeloid leukemia (AML) is a clonal disorder of hematopoietic progenitor cell. In AML, a mutation in FLT3 is commonly occurs and is associated with poor prognosis. We have previously reported that thieno [2,3-d]pyrimidine derivative compound 1 exhibited better antiproliferative activity against MV4-11 cells which harbor mutant FLT3 than AC220, which is a well-known FLT3 inhibitor, and has good microsomal stability. However, compound 1 had poor solubility. We then carried out further structural modification at the C-2 and the C-6 positions of thieno[2,3-d]pyrimidine scaffold. Compound 13b, which possesses a thiazole moiety at the C-2 position, exhibited better antiproliferative activity than compound 1 and showed increased solubility and moderate microsomal stability. These results indicate that compound 13b could be a promising potential FLT inhibitor for AML chemotherapy. (C) 2016 Elsevier Ltd. All rights reserved.
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