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Publikationer i urvalet

12 träffar

Bibliografisk träff 2024-09-11

Discovery of TYRA-300: First Oral Selective FGFR3 Inhibitor for the Treatment of Urothelial Cancers and Achondroplasia.

Hudkins RL, Allen E, Balcer A, Hoffman ID, Iyer S, Neal M, Nelson KJ, Rideout M, Ye Q, Starrett JH, Patel P, Harris T, Swanson RV, Bensen DC.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.4c01531

Bibliografisk träff 2024-06-18

Design, synthesis and antitumor activity of a novel FGFR2-selective degrader to overcome resistance of the FGFR2V564F gatekeeper mutation based on a pan-FGFR inhibitor.

Hu Z, Zhang Q, Li Z, Yang H, Chen X, Zhang Q, Yang T, He X, Feng Q, He J, Yu L.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2024.116612

Bibliografisk träff 2023-07-07

Design, synthesis and biological evaluation of indazole derivatives as selective covalent inhibitors of FGFR4 in wild-type and gatekeeper mutants.

Yang Y, He X, Li Z, Ran K, Wang N, Zhao L, Liu Z, Zeng J, Chang B, Feng Q, Zhang Q, Yu L.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2023.115628

Bibliografisk träff 2022-12-08

Discovery of 2-Amino-7-sulfonyl-7H-pyrrolo[2,3-d]pyrimidine Derivatives as Potent Reversible FGFR Inhibitors with Gatekeeper Mutation Tolerance: Design, Synthesis, and Biological Evaluation.

Xie W, Yang S, Liang L, Wang M, Zuo W, Lei Y, Zhang Y, Tang W, Lu T, Chen Y, Jiang Y.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.2c01420

Bibliografisk träff 2022-11-17

Targeting Gatekeeper Mutations for Kinase Drug Discovery.

Zhou Y, Xiang S, Yang F, Lu X.

J Med Chem · research support, non-u.s. gov't; review; journal article · DOI 10.1021/acs.jmedchem.2c01361

Bibliografisk träff 2022-05-29

Discovery of 1,6-Naphthyridin-2(1H)-one Derivatives as Novel, Potent, and Selective FGFR4 Inhibitors for the Treatment of Hepatocellular Carcinoma.

Zhang X, Wang Y, Ji J, Si D, Bao X, Yu Z, Zhu Y, Zhao L, Li W, Liu J.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.1c01977

Bibliografisk träff 2022-03-10

Design, Synthesis, and Biological Evaluation of Aminoindazole Derivatives as Highly Selective Covalent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR4.

Shao M, Chen X, Yang F, Song X, Zhou Y, Lin Q, Fu Y, Ortega R, Lin X, Tu Z, Patterson AV, Smaill JB, Chen Y, Lu X.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.2c00096

Bibliografisk träff 2021-04-26

Design, synthesis and biological evaluations of a series of Pyrido[1,2-a]pyrimidinone derivatives as novel selective FGFR inhibitors.

Ran K, Zeng J, Wan G, He X, Feng Z, Xiang W, Wei W, Hu X, Wang N, Wang N, Liu Z, Yu L.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2021.113499

Bibliografisk träff 2020-10-01

Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.

Fairhurst RA, Knoepfel T, Buschmann N, Leblanc C, Mah R, Todorov M, Nimsgern P, Ripoche S, Niklaus M, Warin N, Luu VH, Madoerin M, Wirth J, Graus-Porta D, Weiss A, Kiffe M, Wartmann M, Kinyamu-Akunda J, Sterker D, Stamm C, Adler F, Buhles A, Schadt H, Couttet P, Blank J, Galuba I, Trappe J, Voshol J, Ostermann N, Zou C, Berghausen J, Del Rio Espinola A, Jahnke W, Furet P.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.0c01019

Bibliografisk träff 2018-11-16

Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects.

Lu X, Chen H, Patterson AV, Smaill JB, Ding K.

J Med Chem · research support, non-u.s. gov't; review; journal article · DOI 10.1021/acs.jmedchem.8b01531

Bibliografisk träff 2018-03-16

Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors.

Wang Y, Li L, Fan J, Dai Y, Jiang A, Geng M, Ai J, Duan W.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.7b01843

Bibliografisk träff 2016-07-06

Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation.

Yan W, Wang X, Dai Y, Zhao B, Yang X, Fan J, Gao Y, Meng F, Wang Y, Luo C, Ai J, Geng M, Duan W.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.6b00056

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Publikationer i urvalet

Discovery of TYRA-300: First Oral Selective FGFR3 Inhibitor for the Treatment of Urothelial Cancers and Achondroplasia.

Design, synthesis and antitumor activity of a novel FGFR2-selective degrader to overcome resistance of the FGFR2<sup>V564F</sup> gatekeeper mutation based on a pan-FGFR inhibitor.

Design, synthesis and biological evaluation of indazole derivatives as selective covalent inhibitors of FGFR4 in wild-type and gatekeeper mutants.

Discovery of 2-Amino-7-sulfonyl-7<i>H</i>-pyrrolo[2,3-<i>d</i>]pyrimidine Derivatives as Potent Reversible FGFR Inhibitors with Gatekeeper Mutation Tolerance: Design, Synthesis, and Biological Evaluation.

Targeting Gatekeeper Mutations for Kinase Drug Discovery.

Discovery of 1,6-Naphthyridin-2(1<i>H</i>)-one Derivatives as Novel, Potent, and Selective FGFR4 Inhibitors for the Treatment of Hepatocellular Carcinoma.

Design, Synthesis, and Biological Evaluation of Aminoindazole Derivatives as Highly Selective Covalent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR4.

Design, synthesis and biological evaluations of a series of Pyrido[1,2-a]pyrimidinone derivatives as novel selective FGFR inhibitors.

Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.

Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects.

Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors.

Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation.