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Asymmetric synthesis of potent and orally bioavailable thiophene-based EZH2 inhibitors.

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Title: Asymmetric synthesis of potent and orally bioavailable thiophene-based EZH2 inhibitors.
Authors: Tian X; GSK, Research and Development, 1250 South Collegeville Road, Collegeville, PA 19426, United States. Electronic address: Xinrong.2.tian@gsk.com., Newlander K; GSK, Research and Development, 1250 South Collegeville Road, Collegeville, PA 19426, United States., LaFrance L; GSK, Research and Development, 1250 South Collegeville Road, Collegeville, PA 19426, United States., Mack J; GSK, Research and Development, 1250 South Collegeville Road, Collegeville, PA 19426, United States., Brackley J; GSK, Research and Development, 1250 South Collegeville Road, Collegeville, PA 19426, United States., McHugh C; GSK, Research and Development, 1250 South Collegeville Road, Collegeville, PA 19426, United States., He Y; GSK, Research and Development, 1250 South Collegeville Road, Collegeville, PA 19426, United States., Johnson N; GSK, Research and Development, 1250 South Collegeville Road, Collegeville, PA 19426, United States., Truong M; GSK, Research and Development, 1250 South Collegeville Road, Collegeville, PA 19426, United States., Pappalardi MB; GSK, Research and Development, 1250 South Collegeville Road, Collegeville, PA 19426, United States., McCabe MT; GSK, Research and Development, 1250 South Collegeville Road, Collegeville, PA 19426, United States., Knight SD; GSK, Research and Development, 1250 South Collegeville Road, Collegeville, PA 19426, United States.
Source: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2025 Nov 01; Vol. 127, pp. 130291. Date of Electronic Publication: 2025 May 30.
Publication Type: Journal Article
Journal Info: Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3405 (Electronic) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE
Database: MEDLINE Ultimate
Description
ISSN:1464-3405
DOI:10.1016/j.bmcl.2025.130291