SYNTHESIS & EVAL OF 1,5,6 TRIAZACHRYSENE & 5,6,11 TRIAZACHRYSENE DERIVATIVES

合成

基本信息

批准号：
8361326
负责人：
EDMOND J LAVOIE
金额：
$ 0.22万
依托单位：
WASHINGTON UNIVERSITY
依托单位国家：
美国
项目类别：
财政年份：
2011
资助国家：
美国
起止时间：
2011-01-01 至 2011-12-31
项目状态：
已结题

来源：
https://reporter.nih.gov/project-details/8361326
关键词：
Binding Chemotherapy-Oncologic Procedure Clinic Clinical Development Funding Future G-Quartets Grant Isoenzymes Laboratories Lead Malignant Neoplasms Mass Spectrum Analysis National Center for Research Resources Pharmacologic Substance Principal Investigator Research Research Infrastructure Resources Source Topoisomerase II Type I DNA Topoisomerases United States National Institutes of Health antitumor agent biomedical resource chemotherapeutic agent cost design improved interest novel

Binding Chemotherapy-Oncologic Procedure Clinic Clinical Development Funding Future G-Quartets Grant Isoenzymes Laboratories Lead Malignant Neoplasms Mass Spectrum Analysis National Center for Research Resources Pharmacologic Substance Principal Investigator Research Research Infrastructure Resources Source Topoisomerase II Type I DNA Topoisomerases United States National Institutes of Health antitumor agent biomedical resource chemotherapeutic agent cost design improved interest novel

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项目摘要

This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. Primary support for the subproject and the subproject's principal investigator may have been provided by other sources, including other NIH sources. The Total Cost listed for the subproject likely represents the estimated amount of Center infrastructure utilized by the subproject, not direct funding provided by the NCRR grant to the subproject or subproject staff. Our primary research interests are in the discovery and the development of novel pharmaceuticals. For several years our research group has focused on the design and synthesis of novel non-camptothecin topoisomerase I-targeting antitumor agents. Several potent topoisomerase I-targeting agents have been identified. Studies are in progress to identify among these compounds the more promising candidates for development into the clinic. Recently, studies in our laboratory have been undertaken to develop agents that will selectively bind and stabilize G-quadruplex DNA. We are presently exploring the promise and full potential of these G-quadruplex stabilizers in cancer chemotherapy. In addition, our research group has initiated research into the discovery of new lead compounds for the development of isozyme specific topoisomerase II-targeting agents for the future development of an improved clinical agent within this class of cancer chemotherapeutic agents. See more at http://medchem.rutgers.edu/lavoie.shtml

该副本是利用资源的众多研究子项目之一由NIH/NCRR资助的中心赠款提供。对该子弹的主要支持而且，副投影的主要研究员可能是其他来源提供的包括其他NIH来源。列出的总费用可能代表subproject使用的中心基础架构的估计量， NCRR赠款不直接向子弹或副本人员提供的直接资金。我们的主要研究兴趣是新型药物的发现和开发。几年来，我们的研究小组一直集中在新型非膜片蛋白酶组酶I靶向抗肿瘤剂的设计和合成上。已经确定了几种有效的拓扑异构酶I靶向剂。正在进行研究以确定这些化合物中更有希望的候选人开发诊所的候选者。最近，我们在实验室进行了研究，以开发将有选择地结合和稳定G-四链体DNA的药物。目前，我们正在探索这些G四链体稳定剂在癌症化学疗法中的希望和全部潜力。此外，我们的研究小组还开始研究发现新的铅化合物，以开发同工酶特异性拓扑异构酶II靶向剂，以未来开发这类癌症化学治疗剂中改善的临床剂。请参阅http://medchem.rutgers.edu/lavoie.shtml的更多信息