Structural modifications at the 6-position of thieno[2,3-d]pyrimidines and their effects on potency at FLT3 for treatment of acute myeloid leukemia
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- 作者：Hyuntae Kima ; b ; Chulho Leea ; b ; Jee Sun Yanga ; b ; Seonghwi Choia ; b ; Chun-Ho Parkc ; Jong Soon Kangd ; Soo Jin Ohd ; Jieun Yund ; Myung-Hwa Kime ; Gyoonhee Hana ; b ; gyoonhee@yonsei.ac.kr" class="auth_mail" title="E-mail the corresponding author
- 关键词：Fms-like tyrosine kinase 3 (FLT3) ; Acute myeloid leukemia (AML) ; Thieno[2 ; 3-d]pyrimidine ; Metabolic stability
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：14 September 2016
- 年：2016
- 卷：120
- 期：Complete
- 页码：74-85
- 全文大小：1374 K
文摘
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Thieno[2,3-d]pyrimidine derivatives were synthesized and evaluated for FLT3 inhibition.
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Thieno[2,3-d]pyrimidine derivative 16d effectively inhibited FLT3.
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16d also showed antiproliferative activity against leukemia cells and enhanced metabolic stability.
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16d is a promising compound for development as a FLT3 inhibitor.