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Optimization and Investigation of Cruentaren A analogs

Optimization and Investigation of Cruentaren A analogs
Cruentaren A 类似物的优化和研究
批准号：
10078544
负责人：
Brian S J Blagg
金额：
$35.3万
依托单位：
UNIVERSITY OF NOTRE DAME
依托单位国家：
美国
项目类别：
财政年份：
2018
资助国家：
美国
项目状态：
已结题
起止时间：
2018-01-01 至 2022-06-30
来源：
https://reporter.nih.gov/project-details/10078544
关键词：
Animal Cancer ModelAntineoplastic AgentsBindingBinding SitesCancer cell lineCardiotoxicityCell LineCell modelClientClinicalClinical TrialsComplexDataDevelopmentDoseEnergy MetabolismEnzymesExhibitsFrequenciesGenerationsGoalsHSP 90 inhibitionHeat shock proteinsHeat-Shock ResponseHepatotoxicityIn VitroIndividualInvestigationLeadMalignant NeoplasmsMaximum Tolerated DoseMethodsMolecular ChaperonesMolecular ConformationN-terminalNatural ProductsNormal CellPathway interactionsPatientsPeripheral Nervous System DiseasesPharmaceutical PreparationsPreclinical Drug DevelopmentProductionProtein IsoformsProteinsReportingScheduleSignal TransductionStructureStructure-Activity RelationshipTimeToxic effectTranslatingTranslationsWarburg Effectanaloganticancer activityantitumor agentbasecancer cellcancer therapyclinical applicationclinical candidatein vitro activityin vivoin vivo Modelin vivo evaluationinhibitor/antagonistnanomolarneoplastic cellnovelnovel anticancer drugnovel lead compoundoverexpressionpre-clinicalpreclinical developmentpreclinical evaluationprotein degradationprotein foldingresearch clinical testingside effectsmall moleculetumor

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Abstract The development of new methods to treat cancer is greatly needed. In this application, we have identified a macrocyclic small molecule that exhibits high differential selectivity for cancer cells vs. normal cells and aim to develop more simplified analogs of this molecule in an effort to maximize efficiency as well as to decrease the overall number of steps, which will likely lead to clinically useful molecules for the treatment of cancer. In addition, we aim to interrogate the activity manifested by these compounds in both cellular and animal models of cancer, with the goal of providing preclinical data to support the use of such compounds for translational development.
期刊论文(3)
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会议论文
Engineering the Next Generation of Safer Hsp90 Inhibitors
  • 批准号：
    10587304
  • 项目类别：
  • 资助金额：
    $46.33万
  • 财政年份：
    2023
  • 负责人：
    Brian S J Blagg
  • 依托单位：
    UNIVERSITY OF NOTRE DAME
Development and Evaluation of Purine and Coumarin Based Hsp90 Inhibitors
  • 批准号：
    9514012
  • 项目类别：
  • 资助金额：
    $35.33万
  • 财政年份：
    2018
  • 负责人：
    Brian S J Blagg
  • 依托单位：
    UNIVERSITY OF NOTRE DAME
Hsp90B in Bladder Cancer
  • 批准号：
    9922232
  • 项目类别：
  • 资助金额：
    $35.17万
  • 财政年份：
    2018
  • 负责人：
    Brian S J Blagg
  • 依托单位：
    UNIVERSITY OF NOTRE DAME
Optimization and Investigation of Cruentaren A analogs
  • 批准号：
    9902368
  • 项目类别：
  • 资助金额：
    $35.3万
  • 财政年份：
    2018
  • 负责人：
    Brian S J Blagg
  • 依托单位：
    UNIVERSITY OF NOTRE DAME
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