An article Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3) WOS:000604903800035 published article about TYROSINE KINASE INHIBITOR; BREAST-CANCER; FAMILY; JNJ-42756493; ERDAFITINIB; DERIVATIVES; ABERRATIONS; ACTIVATION; MUTATIONS; PROGNOSIS in [Yamani, Abdellah; Lipner, Joanna; Piorkowska, Natalia; Olejkowska, Patrycja; Magdycz, Marta; Dubiel, Krzysztof] Celon Pharma SA, Med Chem Dept, Mokra 41A, PL-05092 Kielpin, Lomianki, Poland; [Zdzalik-Bielecka, Daria; Stanczak, Aleksandra; Stanczak, Paulina Seweryna; Hucz-Kalitowska, Joanna; Dzwonek, Karolina; Lamparska-Przybysz, Monika; Popiel, Delfina; Pieczykolan, Jerzy; Wieczorek, Maciej] Celon Pharma SA, Preclin Dev Dept, Mokra 41A, PL-05092 Kielpin, Lomianki, Poland; [Stanczak, Aleksandra; Wieczorek, Maciej] Celon Pharma SA, Clin Trials Dept, Ogrodowa 2A, PL-05092 Kielpin, Lomianki, Poland; [Lamparska-Przybysz, Monika] Polpharma, Bobrowiecka 6, PL-00728 Warsaw, Poland; [Zdzalik-Bielecka, Daria] Int Inst Mol & Cell Biol, Lab Cell Biol, Warsaw, Poland; [Lipner, Joanna; Magdycz, Marta] Pikralida Sp Zoo, Bukowska 70, PL-60812 Poznan, Poland; [Stanczak, Paulina Seweryna] OncoArendi Therapeut, Zwirki & Wigury 101, Warsaw, Poland in 2021, Cited 56. The Name is 1,3-Dimethoxybenzene. Through research, I have a further understanding and discovery of 151-10-0. Application In Synthesis of 1,3-Dimethoxybenzene
The FGFR family is characterized by four receptors (FGFR 1-4), binding to 18 ligands called fibroblast growth factors (FGFs). Aberrant activation of FGFs and their FGFRs has been implicated in a broad spectrum of human tumors. We employed the scaffolds hybridization approach, scaffold-hopping concept to synthesize a series of novel pyrazole-benzimidazole derivatives 56 (a-x). Compound 56q (CPL304110) was identified as a selective and potent pan-FGFR inhibitor for FGFR1, -2, -3 with IC(50)s of 0.75 nM, 0.50 nM, 3.05 nM respectively, whereas IC50 of 87.90 nM for FGFR4. Due to its favorable pharmacokinetic profile, low toxicity and potent anti-tumor activity in vivo, compound 56q is currently under evaluation in phase I clinical trial for the treatment of bladder, gastric and squamous cell lung cancers (01FGFR2018; NCT04149691). (C) 2020 Elsevier Masson SAS. All rights reserved.
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Reference:
Isothiazole – Wikipedia,
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