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RESEARCH Protein Kinase Inhibitors FGFR1 Inhibitors N-phenylthieno[2,3-d]pyrimidin-4-amines


Thienopyrimidine derivatives have attracted great interest as protein kinase inhibitors over the past years. They were found to be active against VEGFR, EGFR, Aurora kinase, Tie-2, Tpl2, B-Raf and CK2. Also, thieno[3,2-d]pyrimidines were reported as inhibitors of FGFR . The most active FGFR inhibitor has IC50 value of 1.8 μM. Based on the facts that the thienopyrimidines showed some FGFR1 inhibitory activity and known as protein kinases inhibitors we prompted to investigate their inhibitory activity against FGFR1 kinase. Using rational design approach we have found submicromolar inhibitors of FGFR1. The most active compounds, 3-({6-phelthieno[2,3-d]pyrimidin-4-yl}amino)phenol and 3-({5-phenylthieno[2,3-d]pyrimidin-4-yl}amino)phenol have IC50 0.16 and 0.18 μM, respectively.

fgfr1 im1
Figure 1. Thienopyrimidine inhibitor of FGFR1.

  • A.A. Gryshchenko, V.G. Bdzhola, A.O. Balanda, N.V. Briukhovetska, I.M. Kotey, A.G. Golub, T.P. Ruban, L.L. Lukash, S.M. Yarmoluk. (2015) Design, synthesis and biological evaluation of N-phenylthieno[2,3-d]pyrimidin-4-amines as inhibitors of FGFR1. Bioorg Med Chem 23(9):2287-2293.

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