SYNTHETIC STUDIES ON TUMOR PROMOTERS & INHIBITORS

这个子项目是许多利用 由NIH/NCRR资助的中心赠款提供的资源。子项目和 研究者（PI）可能从另一个NIH来源获得了主要资金， 因此可在其他CRISP条目中表示。所列机构为 研究中心，而研究中心不一定是研究者所在的机构。 该项目有五个具体目标：gnidimacrin的合成，gnidimacrin是一种基于PKC靶向治疗癌症的有效先导药物;开发一种通用和灵活的途径，以获得瑞香烷家族的抗癌先导药物并研究其活性;瑞香烷-惕各烷杂合物的合成和生物学评价; laulimalide类似物的合成和生物学评价，laulimalide类似物是对紫杉醇耐药性癌症具有活性的化合物;药物和探针转运蛋白的设计、合成和评价，涉及真实的时间生物发光测定，特别关注转运蛋白缀合物，其被设计用于基于细胞外酶的激活的选择性细胞或组织进入。

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. This project is directed at five specific aims: the synthesis of gnidimacrin, a potent lead for the treatment of cancer based on PKC targeting; the development of a general and flexible rout to anticancer leads in the daphnane family and study of their activity; the synthesis and biological evaluation of daphnane-tigliane hybrids; the synthesis and biological evaluation of laulimalide analogs, compounds active against taxol resistant cancers; the design, synthesis, and evaluation of drug and probe transporters involving a real time bioluminescence assay with a specific focus on transporter conjugates that are designed for selective cell or tissue entry based on activation by extracellular poteases.