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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.

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Title: 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.
Authors: Johannes JW; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Balazs A; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Barratt D; Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 OWG, U.K., Bista M; Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 OWG, 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 CB4 OWG, U.K., Critchlow SE; Bioscience, Oncology R&D, AstraZeneca, Cambridge CB4 OWG, 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 CB4 OWG, U.K., Edmondson SD; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Embrey K; Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 OWG, 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; Oncology Safety, Clinical Pharmacology and Safety Sciences, R&D, AstraZeneca, Cambridge CB4 OWG, U.K., Gunnarsson A; Discovery Sciences, R&D Gothenburg, AstraZeneca, KJ2, 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 CB4 OWG, U.K., Hemsley P; Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 OWG, U.K., Illuzzi G; Bioscience, Oncology R&D, AstraZeneca, Cambridge CB4 OWG, U.K., Lane J; Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 OWG, U.K., Larner C; Oncology Safety, Clinical Pharmacology and Safety Sciences, R&D, AstraZeneca, Cambridge CB4 OWG, U.K., Leo E; Bioscience, Oncology R&D, AstraZeneca, Cambridge CB4 OWG, 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 CB4 OWG, U.K., Martin S; DMPK, Oncology R&D, AstraZeneca, Cambridge CB4 OWG, U.K., McWilliams L; Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 OWG, U.K., O'Connor MJ; Bioscience, Oncology R&D, AstraZeneca, Cambridge CB4 OWG, U.K., Orme JP; Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 OWG, 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 CB4 OWG, 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 CB4 OWG, U.K., Schimpl M; Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 OWG, 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 CB4 OWG, U.K., Talbot V; Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 OWG, U.K., Underwood E; Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 OWG, 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] 2021 Oct 14; Vol. 64 (19), pp. 14498-14512. Date of Electronic Publication: 2021 Sep 27.
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
Description
ISSN:1520-4804
DOI:10.1021/acs.jmedchem.1c01012