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157 results

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Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.
Kettle JG, Anjum R, Barry E, Bhavsar D, Brown C, Boyd S, Campbell A, Goldberg K, Grondine M, Guichard S, Hardy CJ, Hunt T, Jones RDO, Li X, Moleva O, Ogg D, Overman RC, Packer MJ, Pearson S, Schimpl M, Shao W, Smith A, Smith JM, Stead D, Stokes S, Tucker M, Ye Y. Kettle JG, et al. Among authors: anjum r. J Med Chem. 2018 Oct 11;61(19):8797-8810. doi: 10.1021/acs.jmedchem.8b00938. Epub 2018 Sep 24. J Med Chem. 2018. PMID: 30204441
The Pharmacokinetic-Pharmacodynamic (PKPD) Relationships of AZD3229, a Novel and Selective Inhibitor of KIT, in a Range of Mouse Xenograft Models of GIST.
Pilla Reddy V, Anjum R, Grondine M, Smith A, Bhavsar D, Barry E, Guichard SM, Shao W, Kettle JG, Brown C, Banks E, Jones RDO. Pilla Reddy V, et al. Among authors: anjum r. Clin Cancer Res. 2020 Jul 15;26(14):3751-3759. doi: 10.1158/1078-0432.CCR-19-2848. Epub 2020 Mar 27. Clin Cancer Res. 2020. PMID: 32220888
Discovery and pharmacological characterization of AZD3229, a potent KIT/PDGFRα inhibitor for treatment of gastrointestinal stromal tumors.
Banks E, Grondine M, Bhavsar D, Barry E, Kettle JG, Reddy VP, Brown C, Wang H, Mettetal JT, Collins T, Adeyemi O, Overman R, Lawson D, Harmer AR, Reimer C, Drew L, Packer MJ, Cosulich S, Jones RD, Shao W, Wilson D, Guichard S, Fawell S, Anjum R. Banks E, et al. Among authors: anjum r. Sci Transl Med. 2020 Apr 29;12(541):eaaz2481. doi: 10.1126/scitranslmed.aaz2481. Sci Transl Med. 2020. PMID: 32350132
Improving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors.
Degorce SL, Aagaard A, Anjum R, Cumming IA, Diène CR, Fallan C, Johnson T, Leuchowius KJ, Orton AL, Pearson S, Robb GR, Rosen A, Scarfe GB, Scott JS, Smith JM, Steward OR, Terstiege I, Tucker MJ, Turner P, Wilkinson SD, Wrigley GL, Xue Y. Degorce SL, et al. Among authors: anjum r. Bioorg Med Chem. 2020 Dec 1;28(23):115815. doi: 10.1016/j.bmc.2020.115815. Epub 2020 Oct 15. Bioorg Med Chem. 2020. PMID: 33091850
Discovery of a Series of 5-Azaquinazolines as Orally Efficacious IRAK4 Inhibitors Targeting MyD88L265P Mutant Diffuse Large B Cell Lymphoma.
Degorce SL, Anjum R, Bloecher A, Carbajo RJ, Dillman KS, Drew L, Halsall CT, Lenz EM, Lindsay NA, Mayo MF, Pink JH, Robb GR, Rosen A, Scott JS, Xue Y. Degorce SL, et al. Among authors: anjum r. J Med Chem. 2019 Nov 14;62(21):9918-9930. doi: 10.1021/acs.jmedchem.9b01346. Epub 2019 Nov 1. J Med Chem. 2019. PMID: 31622099
Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.
Huang WS, Liu S, Zou D, Thomas M, Wang Y, Zhou T, Romero J, Kohlmann A, Li F, Qi J, Cai L, Dwight TA, Xu Y, Xu R, Dodd R, Toms A, Parillon L, Lu X, Anjum R, Zhang S, Wang F, Keats J, Wardwell SD, Ning Y, Xu Q, Moran LE, Mohemmad QK, Jang HG, Clackson T, Narasimhan NI, Rivera VM, Zhu X, Dalgarno D, Shakespeare WC. Huang WS, et al. Among authors: anjum r. J Med Chem. 2016 May 26;59(10):4948-64. doi: 10.1021/acs.jmedchem.6b00306. Epub 2016 May 12. J Med Chem. 2016. PMID: 27144831
Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88L265P Diffuse Large B-Cell Lymphoma.
Scott JS, Degorce SL, Anjum R, Culshaw J, Davies RDM, Davies NL, Dillman KS, Dowling JE, Drew L, Ferguson AD, Groombridge SD, Halsall CT, Hudson JA, Lamont S, Lindsay NA, Marden SK, Mayo MF, Pease JE, Perkins DR, Pink JH, Robb GR, Rosen A, Shen M, McWhirter C, Wu D. Scott JS, et al. Among authors: anjum r. J Med Chem. 2017 Dec 28;60(24):10071-10091. doi: 10.1021/acs.jmedchem.7b01290. Epub 2017 Dec 11. J Med Chem. 2017. PMID: 29172502
A pharmacokinetic-pharmacodynamic model for the MET tyrosine kinase inhibitor, savolitinib, to explore target inhibition requirements for anti-tumour activity.
Jones RDO, Grondine M, Borodovsky A, San Martin M, DuPont M, D'Cruz C, Schuller A, Henry R, Barry E, Castriotta L, Anjum R, Petersson K, Sahota T, Ahmed GF. Jones RDO, et al. Among authors: anjum r. Br J Pharmacol. 2021 Feb;178(3):600-613. doi: 10.1111/bph.15301. Epub 2020 Dec 7. Br J Pharmacol. 2021. PMID: 33125717 Free article.
Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4.
Degorce SL, Anjum R, Dillman KS, Drew L, Groombridge SD, Halsall CT, Lenz EM, Lindsay NA, Mayo MF, Pink JH, Robb GR, Scott JS, Stokes S, Xue Y. Degorce SL, et al. Among authors: anjum r. Bioorg Med Chem. 2018 Feb 15;26(4):913-924. doi: 10.1016/j.bmc.2018.01.008. Epub 2018 Jan 17. Bioorg Med Chem. 2018. PMID: 29398441
Oncogenic switch and single-agent MET inhibitor sensitivity in a subset of EGFR-mutant lung cancer.
Eser PÖ, Paranal RM, Son J, Ivanova E, Kuang Y, Haikala HM, To C, Okoro JJ, Dholakia KH, Choi J, Eum Y, Ogino A, Missios P, Ercan D, Xu M, Poitras MJ, Wang S, Ngo K, Dills M, Yanagita M, Lopez T, Lin M, Tsai J, Floch N, Chambers ES, Heng J, Anjum R, Santucci AD, Michael K, Schuller AG, Cross D, Smith PD, Oxnard GR, Barbie DA, Sholl LM, Bahcall M, Palakurthi S, Gokhale PC, Paweletz CP, Daley GQ, Jänne PA. Eser PÖ, et al. Among authors: anjum r. Sci Transl Med. 2021 Sep;13(609):eabb3738. doi: 10.1126/scitranslmed.abb3738. Epub 2021 Sep 1. Sci Transl Med. 2021. PMID: 34516823 Free PMC article.
157 results