Co-reporter:Kai Liu and Shijun Zhang
ACS Medicinal Chemistry Letters 2015 Volume 6(Issue 8) pp:894
Publication Date(Web):July 10, 2015
DOI:10.1021/acsmedchemlett.5b00158
Carbazoles represent a family of tricyclic compounds that widely appeared in nature. Numerous studies have revealed a diverse array of bioactivity associated with this scaffold. In the present study, a novel and highly efficient methodology for preparing 1,3-dihydroxy-2-carboxycarbazole from indole-3-acetic acid and Meldrum’s acid was developed. Furthermore, biological characterization demonstrated that this multisubstituted carbazole analogue exhibited inhibitory activity on Aβ aggregation, antioxidative properties, and promising neuroprotective activities in a cellular model of Alzheimer’s disease, thus further supporting the valuable application of this synthetic methodology in search for effective neuroprotectants.Keywords: antioxidant; Aβ oligomers; Carbazole derivative; Meldrum’s acid; neuroprotection; synthesis
Co-reporter:Kai Liu, Shijun Zhang
Tetrahedron Letters 2014 Volume 55(Issue 40) pp:5566-5569
Publication Date(Web):1 October 2014
DOI:10.1016/j.tetlet.2014.08.064
Hydrogen sulfide (H2S) has been recently recognized as an important signaling molecule in biological systems. Herein, we report the development of a fluorescence turn-on probe based on the structure of pomalidomide, a FDA approved drug for the treatment of multiple myeloma. Various characterizations demonstrated high selectivity and sensitivity of this probe toward H2S. Furthermore, the application of this probe to detect H2S in living cells was confirmed by flow cytometry and fluorescence imaging studies.