Kanwar Ankush, Eduful Benjamin J, Barbeto Linda, Carletti Bonomo Piero, Lemus Andrea, Vesely Brian A, Mutka Tina S, Azhari Ala, Kyle Dennis E, Leahy James W
Department of Chemistry, University of South Florida, CHE 205, 4202 East Fowler Avenue, Tampa, Florida 33620, United States.
Department of Global Health, College of Public Health, University of South Florida, 3720 Spectrum Boulevard, Suite 304, Tampa, Florida 33612, United States.
ACS Med Chem Lett. 2017 Jul 31;8(8):797-801. doi: 10.1021/acsmedchemlett.7b00039. eCollection 2017 Aug 10.
We have determined that tetrahydroindazoles such as show potent activity against , the causative agent of leishmaniasis. While the Hsp90 activity and anticancer properties of have previously been explored, we present here our efforts to optimize their activity against via the synthesis of novel analogues designed to probe the hydrophobic pocket of the protozoan Hsp90 orthologue, specifically through the auspices of functionalization of an amine embedded into the scaffold.
我们已经确定，诸如四氢吲唑类化合物对利什曼病的病原体 显示出强大的活性。虽然此前已经研究了 的热休克蛋白90（Hsp90）活性和抗癌特性，但我们在此展示了我们通过合成新型类似物来优化其对 的活性的努力，这些类似物旨在探测原生动物Hsp90同源物的疏水口袋，特别是通过对嵌入支架中的胺进行功能化来实现。
