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9 results for “FGFR1 inhibitor”
Supplementary material 1 from: Al-Mahadeen MM, Jaber AM, Al-Najjar BO (2024) Design, synthesis and biological evaluation of novel 2-hydroxy-1 H-indene-1,3(2 H)-dione derivatives as FGFR1 inhibitors. Pharmacia 71: 1-9. https://doi.org/10.3897/pharmacia.71.e122127
Design, synthesis and biological evaluation of novel 2-hydroxy-1H-indene-1,3(2H)-dione derivatives as FGFR1 inhibitors
Figure 3 from: Al-Mahadeen MM, Jaber AM, Al-Najjar BO (2024) Design, synthesis and biological evaluation of novel 2-hydroxy-1 H-indene-1,3(2 H)-dione derivatives as FGFR1 inhibitors. Pharmacia 71: 1-9. https://doi.org/10.3897/pharmacia.71.e122127
Figure 3 Stick representation of a. Erdafitinib; b. 7b; c. 9a; d. 9b; e. 9c in grey colour, docked within FGFR1 (PDB ID: 5EW8) binding site (green). Generated by Biovia Discovery Studio visualizer®.
Figure 2 from: Al-Mahadeen MM, Jaber AM, Al-Najjar BO (2024) Design, synthesis and biological evaluation of novel 2-hydroxy-1 H-indene-1,3(2 H)-dione derivatives as FGFR1 inhibitors. Pharmacia 71: 1-9. https://doi.org/10.3897/pharmacia.71.e122127
Figure 2 Solid ribbon representation of FGFR1 (PDB ID: 5EW8) with co-crystal (grey) and re-docked (orange) erdafitinib. Generated by Biovia Discovery Studio visualizer®.
Figure 4 from: Al-Mahadeen MM, Jaber AM, Al-Najjar BO (2024) Design, synthesis and biological evaluation of novel 2-hydroxy-1 H-indene-1,3(2 H)-dione derivatives as FGFR1 inhibitors. Pharmacia 71: 1-9. https://doi.org/10.3897/pharmacia.71.e122127
Figure 4 Dose-response curves of compounds 7b, 9a, 9b and 9c FGFR1 inhibitor. A. Dose-response curve of 7b with IC50 = 3.1 μM; B. Dose-response curve of 9a with IC50 = 5.7 μM; C. Dose-response curve of 9b with IC50 = 3.3 μM; D. Dose-response curve of 9c with IC50 = 4.1 μM.
Scheme 1 from: Al-Mahadeen MM, Jaber AM, Al-Najjar BO (2024) Design, synthesis and biological evaluation of novel 2-hydroxy-1 H-indene-1,3(2 H)-dione derivatives as FGFR1 inhibitors. Pharmacia 71: 1-9. https://doi.org/10.3897/pharmacia.71.e122127
Scheme 1 Synthesis of 2-hydroxy-2-(imidazo[1,5-a]pyridinyl)indene-1,3(2H)-diones.
Figure 1 from: Al-Mahadeen MM, Jaber AM, Al-Najjar BO (2024) Design, synthesis and biological evaluation of novel 2-hydroxy-1 H-indene-1,3(2 H)-dione derivatives as FGFR1 inhibitors. Pharmacia 71: 1-9. https://doi.org/10.3897/pharmacia.71.e122127
Figure 1 ORTEP view of the molecular structure and atom numbering scheme of 9b.
Scheme 2 from: Al-Mahadeen MM, Jaber AM, Al-Najjar BO (2024) Design, synthesis and biological evaluation of novel 2-hydroxy-1 H-indene-1,3(2 H)-dione derivatives as FGFR1 inhibitors. Pharmacia 71: 1-9. https://doi.org/10.3897/pharmacia.71.e122127
Scheme 2 Synthesis of compounds 7–9.
Scheme 3 from: Al-Mahadeen MM, Jaber AM, Al-Najjar BO (2024) Design, synthesis and biological evaluation of novel 2-hydroxy-1 H-indene-1,3(2 H)-dione derivatives as FGFR1 inhibitors. Pharmacia 71: 1-9. https://doi.org/10.3897/pharmacia.71.e122127
Scheme 3 Synthesis of compounds 4–6.
RAPID RESISTANCE TO BET INHIBITORS IS MEDIATED BY FGFR1 IN GLIOBLASTOMA
GEO Series GSE245624. Homo sapiens. 9 samples. Type: Expression profiling by high throughput sequencing.
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