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dc.contributor.authorLee, Hyung Kook-
dc.contributor.authorLee, Yun Suk-
dc.contributor.authorRoh, Eun Joo-
dc.contributor.authorRhim, Hyewhon-
dc.contributor.authorLee, Jae Yeol-
dc.contributor.authorShin, Kye Jung-
dc.date.accessioned2024-01-20T23:00:42Z-
dc.date.available2024-01-20T23:00:42Z-
dc.date.created2021-09-03-
dc.date.issued2008-08-01-
dc.identifier.issn0960-894X-
dc.identifier.urihttps://pubs.kist.re.kr/handle/201004/133244-
dc.description.abstractWe have synthesized and evaluated alpha,alpha'-disubstituted phenylacetate derivatives that were designed as T-type calcium channel blockers. Among them, compound 10e (IC50 = 8.17 +/- 0.48 nM) showed the most potent T-type calcium current blocking activity and higher potency than Mibefradil (IC50 = 1.34 +/- 0.49 mu M). The PK profile and subtype selectivity over L-type calcium channel were satisfied for further animal assay using disease model. (c) 2008 Elsevier Ltd. All rights reserved.-
dc.languageEnglish-
dc.publisherPERGAMON-ELSEVIER SCIENCE LTD-
dc.subjectCA2+ CHANNELS-
dc.subjectMIBEFRADIL-
dc.subjectDISCOVERY-
dc.subjectSECRETION-
dc.subjectCURRENTS-
dc.titleSynthesis and evaluation of alpha,alpha'-disubstituted phenylacetate derivatives for T-type calcium channel blockers-
dc.typeArticle-
dc.identifier.doi10.1016/j.bmcl.2008.06.037-
dc.description.journalClass1-
dc.identifier.bibliographicCitationBIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.18, no.15, pp.4424 - 4427-
dc.citation.titleBIOORGANIC & MEDICINAL CHEMISTRY LETTERS-
dc.citation.volume18-
dc.citation.number15-
dc.citation.startPage4424-
dc.citation.endPage4427-
dc.description.journalRegisteredClassscie-
dc.description.journalRegisteredClassscopus-
dc.identifier.wosid000257986400039-
dc.identifier.scopusid2-s2.0-47949088481-
dc.relation.journalWebOfScienceCategoryChemistry, Medicinal-
dc.relation.journalWebOfScienceCategoryChemistry, Organic-
dc.relation.journalResearchAreaPharmacology & Pharmacy-
dc.relation.journalResearchAreaChemistry-
dc.type.docTypeArticle-
dc.subject.keywordPlusCA2+ CHANNELS-
dc.subject.keywordPlusMIBEFRADIL-
dc.subject.keywordPlusDISCOVERY-
dc.subject.keywordPlusSECRETION-
dc.subject.keywordPlusCURRENTS-
dc.subject.keywordAuthorT-type calcium channel-
dc.subject.keywordAuthorneuropathic pain-
dc.subject.keywordAuthorpatch-clamp-
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