title: Discovery of novel N-substituted carbazoles as neuroprotective agents with potent anti-oxidative activity.
abstract: 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.
authors: 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.
authors: Daqian
authors: D
authors: Zhu
authors: Meihui
authors: M
authors: Chen
authors: Min
authors: M
authors: Li
authors: Bingling
authors: B
authors: Luo
authors: Yang
authors: Y
authors: Zhao
authors: Peng
authors: P
authors: Huang
authors: Fengtian
authors: F
authors: Xue
authors: Simona
authors: S
authors: Rapposelli
authors: Rongbiao
authors: R
authors: Pi
authors: Shijun
authors: S
authors: Wen
mesh_terms: D000818:Animals; D000975:Antioxidants / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002227:Carbazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D055808:Drug Discovery; D051379:Mice; D018696:Neuroprotective Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D009584:Nitrogen / Q000737:chemistry*; D017382:Reactive Oxygen Species
chemical_list: D000975:Antioxidants; D002227:Carbazoles; D018696:Neuroprotective Agents; D017382:Reactive Oxygen Species; D009584:Nitrogen
keywords: AD; Alzheimer's disease; Antioxidant; CNS; Carbazole; HT22 cell; Neuroprotection; ROS; central nerve system; mCPBA; meta-chloroperoxybenzoic acid; reactive oxygen species