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Eur J Med Chem. 2013 Oct;68:81-8. doi: 10.1016/j.ejmech.2013.07.029. Epub 2013 Aug 9.

Discovery of novel N-substituted carbazoles as neuroprotective agents with potent anti-oxidative activity.

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State Key Laboratory of Oncology in South China, Sun Yat-Sen University Cancer Center, Guangzhou 510060, China; School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510006, China.


Carbazole moiety is an important scaffold with a variety of biological applications, for example, anti-oxidative stress. Our previous synthesized carbazoles were screened for their neuroprotective properties against two individual oxidative stresses. Some of the new carbazole derivatives were observed with modest to good neuroprotective effects on neuronal cells HT22 against cell injury induced by glutamate or homocysteic acid (HCA). Substituents introduced to the carbazole ring system play crucial roles in their biological activities. In particular, a bulky group favors the neuroprotective activity of the compounds. One of the new compounds, 6, showed the best neuroprotective effects, which might result from its anti-oxidative activity with a GSH-independent mechanism. These findings might provide an alternative strategy for the development of novel carbazole derivatives for the treatment of CNS diseases such as Alzheimer's disease.


AD; Alzheimer's disease; Antioxidant; CNS; Carbazole; HT22 cell; Neuroprotection; ROS; central nerve system; mCPBA; meta-chloroperoxybenzoic acid; reactive oxygen species

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