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Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs.
Johannes JW, Balazs A, Barratt D, Bista M, Chuba MD, Cosulich S, Critchlow SE, Degorce SL, Di Fruscia P, Edmondson SD, Embrey K, Fawell S, Ghosh A, Gill SJ, Gunnarsson A, Hande SM, Heightman TD, Hemsley P, Illuzzi G, Lane J, Larner C, Leo E, Liu L, Madin A, Martin S, McWilliams L, O'Connor MJ, Orme JP, Pachl F, Packer MJ, Pei X, Pike A, Schimpl M, She H, Staniszewska AD, Talbot V, Underwood E, Varnes JG, Xue L, Yao T, Zhang K, Zhang AX, Zheng X. Johannes JW, et al. Among authors: pike a. J Med Chem. 2021 Oct 14;64(19):14498-14512. doi: 10.1021/acs.jmedchem.1c01012. Epub 2021 Sep 27. J Med Chem. 2021. PMID: 34570508
Optimization of a series of potent, selective and orally bioavailable SYK inhibitors.
Grimster NP, Gingipalli L, Barlaam B, Su Q, Zheng X, Watson D, Wang H, Simpson I, Pike A, Balazs A, Boiko S, Ikeda TP, Impastato AC, Jones NH, Kawatkar S, Kemmitt P, Lamont S, Patel J, Read J, Sarkar U, Sha L, Tomlinson RC, Wang H, Wilson DM, Zehnder TE, Wang L, Wang P, Goldberg FW, Shao W, Fawell S, Dry H, Dowling JE, Edmondson SD. Grimster NP, et al. Among authors: pike a. Bioorg Med Chem Lett. 2020 Oct 1;30(19):127433. doi: 10.1016/j.bmcl.2020.127433. Epub 2020 Jul 24. Bioorg Med Chem Lett. 2020. PMID: 32717371
Identification of a novel series of azabenzimidazole-derived inhibitors of spleen tyrosine kinase.
Kawatkar SP, Barlaam B, Kemmitt P, Simpson I, Watson D, Wang P, Lamont S, Su Q, Boiko S, Ikeda T, Patel J, Pike A, Pollard H, Read J, Sarkar U, Wang H, Wen Q, Yan Z, Dowling JE, Dry H, Edmondson SD. Kawatkar SP, et al. Among authors: pike a. Bioorg Med Chem Lett. 2020 Sep 15;30(18):127393. doi: 10.1016/j.bmcl.2020.127393. Epub 2020 Jul 10. Bioorg Med Chem Lett. 2020. PMID: 32721854
Novel potent and selective pyrazolylpyrimidine-based SYK inhibitors.
Barlaam B, Boiko S, Boyd S, Dry H, Gingipalli L, Ikeda T, Johnson T, Kawatkar S, Lorthioir O, Pike A, Pollard H, Read J, Su Q, Wang H, Wang H, Wang L, Wang P, Edmondson SD. Barlaam B, et al. Among authors: pike a. Bioorg Med Chem Lett. 2020 Nov 15;30(22):127523. doi: 10.1016/j.bmcl.2020.127523. Epub 2020 Aug 30. Bioorg Med Chem Lett. 2020. PMID: 32877741
Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.
Barlaam B, Casella R, Cidado J, Cook C, De Savi C, Dishington A, Donald CS, Drew L, Ferguson AD, Ferguson D, Glossop S, Grebe T, Gu C, Hande S, Hawkins J, Hird AW, Holmes J, Horstick J, Jiang Y, Lamb ML, McGuire TM, Moore JE, O'Connell N, Pike A, Pike KG, Proia T, Roberts B, San Martin M, Sarkar U, Shao W, Stead D, Sumner N, Thakur K, Vasbinder MM, Varnes JG, Wang J, Wang L, Wu D, Wu L, Yang B, Yao T. Barlaam B, et al. Among authors: pike kg, pike a. J Med Chem. 2020 Dec 24;63(24):15564-15590. doi: 10.1021/acs.jmedchem.0c01754. Epub 2020 Dec 11. J Med Chem. 2020. PMID: 33306391
Pyridones in drug discovery: Recent advances.
Zhang Y, Pike A. Zhang Y, et al. Among authors: pike a. Bioorg Med Chem Lett. 2021 Apr 15;38:127849. doi: 10.1016/j.bmcl.2021.127849. Epub 2021 Feb 18. Bioorg Med Chem Lett. 2021. PMID: 33609656 Review.
Diverse, Potent, and Efficacious Inhibitors That Target the EED Subunit of the Polycomb Repressive Complex 2 Methyltransferase.
Bagal SK, Gregson C, O' Donovan DH, Pike KG, Bloecher A, Barton P, Borodovsky A, Code E, Fillery SM, Hsu JH, Kawatkar SP, Li C, Longmire D, Nai Y, Nash SC, Pike A, Robinson J, Read JA, Rawlins PB, Shen M, Tang J, Wang P, Woods H, Williamson B. Bagal SK, et al. Among authors: pike kg, pike a. J Med Chem. 2021 Dec 9;64(23):17146-17183. doi: 10.1021/acs.jmedchem.1c01161. Epub 2021 Nov 22. J Med Chem. 2021. PMID: 34807608
Preclinical Characterization of AZD5305, A Next-Generation, Highly Selective PARP1 Inhibitor and Trapper.
Illuzzi G, Staniszewska AD, Gill SJ, Pike A, McWilliams L, Critchlow SE, Cronin A, Fawell S, Hawthorne G, Jamal K, Johannes J, Leonard E, Macdonald R, Maglennon G, Nikkilä J, O'Connor MJ, Smith A, Southgate H, Wilson J, Yates J, Cosulich S, Leo E. Illuzzi G, et al. Among authors: pike a. Clin Cancer Res. 2022 Nov 1;28(21):4724-4736. doi: 10.1158/1078-0432.CCR-22-0301. Clin Cancer Res. 2022. PMID: 35929986 Free PMC article.
Optimization of a series of novel, potent and selective Macrocyclic SYK inhibitors.
Grimster NP, Gingipalli L, Balazs A, Barlaam B, Boiko S, Boyd S, Dry H, Goldberg FW, Ikeda T, Johnson T, Kawatkar S, Kemmitt P, Lamont S, Lorthioir O, Mfuh A, Patel J, Pike A, Read J, Romero R, Sarkar U, Sha L, Simpson I, Song K, Su Q, Wang H, Watson D, Wu A, Zehnder TE, Zheng X, Li S, Dong Z, Yang D, Song Y, Wang P, Liu X, Dowling JE, Edmondson SD. Grimster NP, et al. Among authors: pike a. Bioorg Med Chem Lett. 2023 Jul 15;91:129352. doi: 10.1016/j.bmcl.2023.129352. Epub 2023 Jun 2. Bioorg Med Chem Lett. 2023. PMID: 37270074
468 results