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Article: Discovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides

TitleDiscovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides
Authors
KeywordsIndazolyl benzenesulfonamide
antimitotic agents
Tyrosine Threonine Kinase (TTK)
Mitotic kinase
Anticancer
Monopolar Spindle 1 kinase (Mps1)
Issue Date2014
Citation
Bioorganic and Medicinal Chemistry, 2014, v. 22, n. 17, p. 4968-4997 How to Cite?
AbstractTTK kinase was identified by in-house siRNA screen and pursued as a tractable, novel target for cancer treatment. A screening campaign and systematic optimization, supported by computer modeling led to an indazole core with key sulfamoylphenyl and acetamido moieties at positions 3 and 5, respectively, establishing a novel chemical class culminating in identification of 72 (CFI-400936). This potent inhibitor of TTK (IC50 = 3.6 nM) demonstrated good activity in cell based assay and selectivity against a panel of human kinases. A co-complex TTK X-ray crystal structure and results of a xenograft study with TTK inhibitors from this class are described. © 2014 Elsevier Ltd. All rights reserved.
Persistent Identifierhttp://hdl.handle.net/10722/292843
ISSN
2023 Impact Factor: 3.3
2023 SCImago Journal Rankings: 0.614
ISI Accession Number ID

 

DC FieldValueLanguage
dc.contributor.authorLaufer, Radoslaw-
dc.contributor.authorNg, Grace-
dc.contributor.authorLiu, Yong-
dc.contributor.authorPatel, Narendra Kumar B.-
dc.contributor.authorEdwards, Louise G.-
dc.contributor.authorLang, Yunhui-
dc.contributor.authorLi, Sze Wan-
dc.contributor.authorFeher, Miklos-
dc.contributor.authorAwrey, Don E.-
dc.contributor.authorLeung, Genie-
dc.contributor.authorBeletskaya, Irina-
dc.contributor.authorPlotnikova, Olga-
dc.contributor.authorMason, Jacqueline M.-
dc.contributor.authorHodgson, Richard-
dc.contributor.authorWei, Xin-
dc.contributor.authorMao, Guodong-
dc.contributor.authorLuo, Xunyi-
dc.contributor.authorHuang, Ping-
dc.contributor.authorGreen, Erin-
dc.contributor.authorKiarash, Reza-
dc.contributor.authorLin, Dan Chi Chia-
dc.contributor.authorHarris-Brandts, Marees-
dc.contributor.authorBan, Fuqiang-
dc.contributor.authorNadeem, Vincent-
dc.contributor.authorMak, Tak W.-
dc.contributor.authorPan, Guohua J.-
dc.contributor.authorQiu, Wei-
dc.contributor.authorChirgadze, Nickolay Y.-
dc.contributor.authorPauls, Henry W.-
dc.date.accessioned2020-11-17T14:57:20Z-
dc.date.available2020-11-17T14:57:20Z-
dc.date.issued2014-
dc.identifier.citationBioorganic and Medicinal Chemistry, 2014, v. 22, n. 17, p. 4968-4997-
dc.identifier.issn0968-0896-
dc.identifier.urihttp://hdl.handle.net/10722/292843-
dc.description.abstractTTK kinase was identified by in-house siRNA screen and pursued as a tractable, novel target for cancer treatment. A screening campaign and systematic optimization, supported by computer modeling led to an indazole core with key sulfamoylphenyl and acetamido moieties at positions 3 and 5, respectively, establishing a novel chemical class culminating in identification of 72 (CFI-400936). This potent inhibitor of TTK (IC50 = 3.6 nM) demonstrated good activity in cell based assay and selectivity against a panel of human kinases. A co-complex TTK X-ray crystal structure and results of a xenograft study with TTK inhibitors from this class are described. © 2014 Elsevier Ltd. All rights reserved.-
dc.languageeng-
dc.relation.ispartofBioorganic and Medicinal Chemistry-
dc.subjectIndazolyl benzenesulfonamide-
dc.subjectantimitotic agents-
dc.subjectTyrosine Threonine Kinase (TTK)-
dc.subjectMitotic kinase-
dc.subjectAnticancer-
dc.subjectMonopolar Spindle 1 kinase (Mps1)-
dc.titleDiscovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides-
dc.typeArticle-
dc.description.naturelink_to_subscribed_fulltext-
dc.identifier.doi10.1016/j.bmc.2014.06.027-
dc.identifier.pmid25043312-
dc.identifier.scopuseid_2-s2.0-84906937206-
dc.identifier.volume22-
dc.identifier.issue17-
dc.identifier.spage4968-
dc.identifier.epage4997-
dc.identifier.eissn1464-3391-
dc.identifier.isiWOS:000341293300047-
dc.identifier.issnl0968-0896-

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