Conformation-Activity Relationships
构象-活性关系
基本信息
- 批准号:7619130
- 负责人:
- 金额:$ 27.96万
- 依托单位:
- 依托单位国家:美国
- 项目类别:
- 财政年份:2000
- 资助国家:美国
- 起止时间:2000-03-01 至 2011-08-31
- 项目状态:已结题
- 来源:
- 关键词:ATP phosphohydrolaseAffectAlkenesAnabolismAnti-Bacterial AgentsAntifungal AgentsAreaAttentionBindingBiologicalBiological AssayBiological FactorsCarbonClassificationCollaborationsComplementComplexComputing MethodologiesDNA Sequence RearrangementDevelopmentEpothilonesEthersEvolutionFermentationFutureGene ClusterGenerationsGlycolsGrantInvestigationLactonesLeadMacrolidesMethodologyMethodsMicrotubule PolymerizationMicrotubulesMinorMitoticModificationMolecularMolecular ConformationMono-SNuclear Magnetic ResonanceOrganismPatternPeripheralPreparationPropertyProteinsPyransReactionResearchResearch PersonnelRouteSkeletonSolutionsStructureStructure-Activity RelationshipStudy SubjectSystemTechniquesTherapeuticanalogapoptolidinchemotherapeutic agentcytotoxicitydesignflexibilityfunctional groupimprovedinsightinterestnovelpeloruside Apharmacophorepreferenceprofessorprogramsspatial relationship
项目摘要
DESCRIPTION (provided by applicant): Our overall program is interested in the fundamental issues regarding the evolution of polyketide natural products. The focus of these studies is from two complementary perspectives. The first deals with specific structural features found in polyketides, their effect on conformation, and the importance of conformation on biological activity. The second perspective focuses on structurally related polyketides and the co-evolution of their protein targets. Polyketide natural products are ideal subjects for these studies due to their complex structure and diverse biological activities which have shown utility towards the study and treatment of a number of therapeutic areas. During the previous research period we have shown that conformation is an important complement to classic structure-activity relationships and provides useful information for the development of future chemotherapeutic agents. As a proof of principle, a conformation-activity relationship study of the microtubule-stabilizing natural products, the epothilones, provided important information with regards to the pharmacophore as well as new leads for further development. During the next grant period, our studies will investigate three fundamentally unique projects, 1. Conformation-activity relationships of peloruside A, 2. a study of the evolutionary relationship between apoptolidin and structurally related plecomacrolides, bafilomycin and concanamycin, and 3. The development of precursor-directed biosynthetic techniques for the preparation of complex polyketide analogues. The complex natural products targeted in this application will be prepared via unique but practical synthetic strategies. Moreover, where appropriate, we have incorporated the development of a number of new synthetic methods for the preparation of complex structural units common to polyketide natural products.
描述(由申请人提供):我们的整体计划是关于聚酮化合物天然产物的演变的基本问题感兴趣。这些研究的重点是从两个互补的角度。第一个涉及到聚酮化合物中发现的特定结构特征,它们对构象的影响,以及构象对生物活性的重要性。第二个视角关注结构相关的聚酮化合物及其蛋白质靶点的共同进化。聚酮化合物天然产物由于其复杂的结构和多样的生物活性而成为这些研究的理想对象,这些生物活性已显示出对许多治疗领域的研究和治疗的效用。在之前的研究期间,我们已经表明构象是经典结构-活性关系的重要补充,并为未来化疗药物的开发提供了有用的信息。作为原理的证明,微管稳定天然产物埃坡霉素的构象-活性关系研究提供了关于药效团的重要信息以及进一步开发的新线索。在下一个赠款期间,我们的研究将调查三个基本独特的项目,1。peloruside A的构象-活性关系,2.一项研究的进化关系之间的martolidin和结构相关的plecomacrolides,巴弗洛霉素和concanamycin,和3。以生物合成技术为导向之合成复杂聚酮化合物。本申请中针对的复杂天然产物将通过独特但实用的合成策略制备。此外,在适当的情况下,我们已经纳入了一些新的合成方法的开发,用于制备聚酮化合物天然产物常见的复杂结构单元。
项目成果
期刊论文数量(3)
专著数量(0)
科研奖励数量(0)
会议论文数量(0)
专利数量(0)
Rapid access to conformational analogues of (+)-peloruside A.
快速获得 ( )-peloruside A 的构象类似物。
- DOI:10.1021/ol203268t
- 发表时间:2012
- 期刊:
- 影响因子:5.2
- 作者:Zhao,Zhiming;Taylor,RichardE
- 通讯作者:Taylor,RichardE
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Richard E. Taylor其他文献
The anti-ischemia agent ranolazine promotes the development of intestinal tumors in APC(Min/+) mice.
抗缺血剂雷诺嗪促进 APC(Min/ ) 小鼠肠道肿瘤的发展。
- DOI:
- 发表时间:
2004 - 期刊:
- 影响因子:9.7
- 作者:
M. Suckow;L. Gutierrez;C. Risatti;W. Wolter;Richard E. Taylor;M. Pollard;R. Navari;F. Castellino;N. Paoni - 通讯作者:
N. Paoni
A Formal Total Synthesis of Epothilone A: Enantioselective Preparation of the C1−C6 and C7−C12 Fragments1
埃坡霉素 A 的正式全合成:C1−C6 和 C7−C12 片段的对映选择性制备1
- DOI:
10.1021/jo981461u - 发表时间:
1998 - 期刊:
- 影响因子:3.6
- 作者:
Richard E. Taylor;G. Galvin;Kerry A. Hilfiker;Yue Chen - 通讯作者:
Yue Chen
Solid-state photochemistry. Remarkable effects of the packing of molecules in crystals on the diastereoselectivity of the intramolecular 2 + 2 photocycloaddition of a 4-(3'-butenyl)-2,5-cyclohexadien-1-one
固态光化学。
- DOI:
10.1021/ja00048a070 - 发表时间:
1992 - 期刊:
- 影响因子:15
- 作者:
A. Schultz;A. Taveras;Richard E. Taylor;F. Tham;R. Kullnig - 通讯作者:
R. Kullnig
Chapter 8 Total synthesis of myriaporones 1, 3, and 4
第 8 章 myriaporones 1、3 和 4 的全合成
- DOI:
- 发表时间:
2005 - 期刊:
- 影响因子:0
- 作者:
Richard E. Taylor;K. N. Fleming;B. Hearn - 通讯作者:
B. Hearn
Die Synthese und biologische Validierung von Desepoxyisotedanolid und dessen Vergleich mit Desepoxytedanolid
去环氧异丁醇的合成和生物验证以及去环氧异丁醇的制备
- DOI:
10.1002/ange.201501526 - 发表时间:
2015 - 期刊:
- 影响因子:0
- 作者:
Arun Naini;Yazh Muthukumar;Aruna Raja;R. Franke;Ian Harrier;Amos B. Smith;Dongjoo Lee;Richard E. Taylor;F. Sasse;M. Kalesse - 通讯作者:
M. Kalesse
Richard E. Taylor的其他文献
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{{ truncateString('Richard E. Taylor', 18)}}的其他基金
Synthesis and Biosynthesis of Pyran and Spiroketal Structural Units
吡喃和螺缩酮结构单元的合成和生物合成
- 批准号:
8270544 - 财政年份:2010
- 资助金额:
$ 27.96万 - 项目类别:
Synthesis and Biosynthesis of Pyran and Spiroketal Structural Units
吡喃和螺缩酮结构单元的合成和生物合成
- 批准号:
8456204 - 财政年份:2010
- 资助金额:
$ 27.96万 - 项目类别:
Synthesis and Biosynthesis of Pyran and Spiroketal Structural Units
吡喃和螺缩酮结构单元的合成和生物合成
- 批准号:
7782483 - 财政年份:2010
- 资助金额:
$ 27.96万 - 项目类别:
Synthesis and Biosynthesis of Pyran and Spiroketal Structural Units
吡喃和螺缩酮结构单元的合成和生物合成
- 批准号:
8068340 - 财政年份:2010
- 资助金额:
$ 27.96万 - 项目类别:
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