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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
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DbLabel: MEDLINE Ultimate
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AccessLevel: 2
PubType: Academic Journal
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  Data: Asymmetric synthesis of potent and orally bioavailable thiophene-based EZH2 inhibitors.
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  Data: <searchLink fieldCode="AU" term="%22Tian+X%22">Tian X</searchLink>; GSK, Research and Development, 1250 South Collegeville Road, Collegeville, PA 19426, United States. Electronic address: Xinrong.2.tian@gsk.com.<br /><searchLink fieldCode="AU" term="%22Newlander+K%22">Newlander K</searchLink>; GSK, Research and Development, 1250 South Collegeville Road, Collegeville, PA 19426, United States.<br /><searchLink fieldCode="AU" term="%22LaFrance+L%22">LaFrance L</searchLink>; GSK, Research and Development, 1250 South Collegeville Road, Collegeville, PA 19426, United States.<br /><searchLink fieldCode="AU" term="%22Mack+J%22">Mack J</searchLink>; GSK, Research and Development, 1250 South Collegeville Road, Collegeville, PA 19426, United States.<br /><searchLink fieldCode="AU" term="%22Brackley+J%22">Brackley J</searchLink>; GSK, Research and Development, 1250 South Collegeville Road, Collegeville, PA 19426, United States.<br /><searchLink fieldCode="AU" term="%22McHugh+C%22">McHugh C</searchLink>; GSK, Research and Development, 1250 South Collegeville Road, Collegeville, PA 19426, United States.<br /><searchLink fieldCode="AU" term="%22He+Y%22">He Y</searchLink>; GSK, Research and Development, 1250 South Collegeville Road, Collegeville, PA 19426, United States.<br /><searchLink fieldCode="AU" term="%22Johnson+N%22">Johnson N</searchLink>; GSK, Research and Development, 1250 South Collegeville Road, Collegeville, PA 19426, United States.<br /><searchLink fieldCode="AU" term="%22Truong+M%22">Truong M</searchLink>; GSK, Research and Development, 1250 South Collegeville Road, Collegeville, PA 19426, United States.<br /><searchLink fieldCode="AU" term="%22Pappalardi+MB%22">Pappalardi MB</searchLink>; GSK, Research and Development, 1250 South Collegeville Road, Collegeville, PA 19426, United States.<br /><searchLink fieldCode="AU" term="%22McCabe+MT%22">McCabe MT</searchLink>; GSK, Research and Development, 1250 South Collegeville Road, Collegeville, PA 19426, United States.<br /><searchLink fieldCode="AU" term="%22Knight+SD%22">Knight SD</searchLink>; GSK, Research and Development, 1250 South Collegeville Road, Collegeville, PA 19426, United States.
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  Data: <searchLink fieldCode="JN" term="%229107377%22">Bioorganic & medicinal chemistry letters</searchLink> [Bioorg Med Chem Lett] 2025 Nov 01; Vol. 127, pp. 130291. <i>Date of Electronic Publication: </i>2025 May 30.
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  Data: <i>Publisher: </i><searchLink fieldCode="PB" term="%22Elsevier+Science+Ltd%22">Elsevier Science Ltd </searchLink><i>Country of Publication: </i>England <i>NLM ID: </i>9107377 <i>Publication Model: </i>Print-Electronic <i>Cited Medium: </i>Internet <i>ISSN: </i>1464-3405 (Electronic) <i>Linking ISSN: </i><searchLink fieldCode="IS" term="%220960894X%22">0960894X </searchLink><i>NLM ISO Abbreviation: </i>Bioorg Med Chem Lett <i>Subsets: </i>MEDLINE
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        Value: 10.1016/j.bmcl.2025.130291
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              Text: 2025 Nov 01
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