Discovery of 6-Fluoro-5-{4-[(5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD9574): A CNS-Penetrant, PARP1-Selective Inhibitor.
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| Title: | Discovery of 6-Fluoro-5-{4-[(5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD9574): A CNS-Penetrant, PARP1-Selective Inhibitor. |
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| Authors: | Johannes JW; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Balazs AYS; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Barratt D; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Bista M; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Chuba MD; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Cosulich S; Oncology Projects, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Critchlow SE; Bioscience, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Degorce SL; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Di Fruscia P; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Edmondson SD; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Embrey KJ; New Modalities & Parenteral Development, Pharmaceutical Technology & Development, Operations, AstraZeneca, Macclesfield SK10 2NA, U.K., Fawell S; Oncology Discovery, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Ghosh A; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Gill SJ; Safety Sciences, Clinical Pharmacology and Safety Sciences R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Gunnarsson A; Discovery Sciences, R&D Gothenburg, AstraZeneca, Pepparedsleden 1, SE-431 83 Mölndal, Sweden., Hande SM; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Heightman TD; Chemistry, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Hemsley P; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Illuzzi G; Bioscience, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Lane J; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Larner CJB; Safety Sciences, Clinical Pharmacology and Safety Sciences R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Leo E; Bioscience, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Liu L; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, P. R. China., Madin A; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., McWilliams L; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., O'Connor MJ; Bioscience, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Orme JP; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Pachl F; Discovery Sciences, R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Packer MJ; Computational Chemistry, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Pei X; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, P. R. China., Pike A; DMPK, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Schimpl M; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., She H; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, P. R. China., Staniszewska AD; Bioscience, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Talbot V; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Underwood E; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Varnes JG; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Xue L; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, P. R. China., Yao T; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, P. R. China., Zhang K; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, P. R. China., Zhang AX; Discovery Sciences, R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Zheng X; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States. |
| Source: | Journal of medicinal chemistry [J Med Chem] 2024 Dec 26; Vol. 67 (24), pp. 21717-21728. Date of Electronic Publication: 2024 Dec 10. |
| Publication Type: | Journal Article |
| Journal Info: | Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE |
| Database: | MEDLINE Ultimate |
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