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

该子项目是利用NIH/NCRR资助的中心赠款提供的资源的许多研究子项目之一。子项目和研究者（PI）可能从另一个NIH来源获得主要资金，因此可以在其他CRISP条目中表示。所列机构为中心，不一定是研究者所在机构。我们的主要研究领域是药物发现和开发。目前的研究包括设计和合成新型拓扑异构酶I和II毒药作为抑制剂。已经鉴定了几种有效的拓扑异构酶毒物，并且正在进行研究以鉴定那些具有更大潜力的毒物作为临床候选物。还对癌症化疗剂六甲基三聚氰胺或六甲蜜胺的类似物及其可疑活性代谢物的前药的合成进行了研究。致癌机制正在通过检查多环芳香族化合物的代谢物在癌症发生和肿瘤生长中的潜在作用来研究。

This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. The subproject and investigator (PI) may have received primary funding from another NIH source, and thus could be represented in other CRISP entries. The institution listed is for the Center, which is not necessarily the institution for the investigator. Our primary areas of research are drug discovery and development. Research currently includes the design and synthesis of novel topoisomerase I and II poisons as antineoplastic agents. Several potent topoisomerase poisons have been identified and studies are in progress to identify those with the greater potential to serve as clinical candidates. Research has also been undertaken on the synthesis of analogs of the cancer chemotherapeutic agent, hexamethylmelamine or Altretamine, as well as prodrugs of its suspect active metabolite. Mechanisms of carcinogenesis are being investigated by examining the potential role of metabolites of polycyclic aromatic compounds in cancer initiation and tumor growth.