Bioorganic and Medicinal Chemistry p. 2053 - 2059 (2016)
Update date:2022-08-05
Topics:
Gryshchenko
Tarnavskiy
Levchenko
Bdzhola
Volynets
Golub
Ruban
Vygranenko
Lukash
Yarmoluk
Fibroblast growth factor receptor 1 (FGFR1) plays an important role in tumorigenesis and is therefore an attractive target for anticancer therapy. Using molecular docking approach we have identified inhibitor of FGFR1 belonging to 5-amino-4-(1H-benzoimidazol-2-yl)-phenyl-1,2-dihydro-pyrrol-3-ones with IC50 value of 3.5 μM. A series of derivatives of this chemical scaffold has been synthesized and evaluated for inhibition of FGFR1 kinase activity. It was revealed that the most promising compounds 5-amino-1-(3-hydroxy-phenyl)-4-(6-methyl-1H-benzoimidazol-2-yl)-1,2-dihydro-pyrrol-3-one and 5-amino-4-(1H-benzoimidazol-2-yl)-1-(3-hydroxy-phenyl)-1,2-dihydro-pyrrol-3-one inhibit FGFR1 with IC50 values of 0.63 and 0.32 μM, respectively, and posses antiproliferative activity against KG1 myeloma cell line with IC50 values of 5.6 and 9.3 μM. Structure-activity relationships have been studied and binding mode of this chemical class has been proposed.
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Doi:10.1016/S0040-4039(01)83598-X
(1977)Doi:10.1021/ol036017e
(2003)Doi:10.1021/ja308623n
(2012)Doi:10.1021/jf60215a035
(1978)Doi:10.1021/jm00199a021
(1978)Doi:10.1016/00404-0399(50)0972F-
(1995)