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Syntheses, neural protective activities, and inhibition of glycogen synthase kinase-3? of substituted quinolines.

ABSTRACT: A new series of fifteen 5-, 6-, and 8-appended 4-methylquinolines were synthesized and evaluated for their neural protective activities. Selected compounds were further examined for their inhibition of glycogen synthase kinase-3? (GSK-3?) and protein kinase C (PKC). Two most potent analogs, compounds 3 and 10, show nanomolar protective activities in amyloid ?-induced MC65 cells and enzymatic inhibitory activities against GSK-3?, but poor PKC inhibitory activities. Using normal mouse model, the distribution of the most potent analog 3 in various tissues and possible toxic effects in the locomotors and inhibition of liver transaminases activities were carried out. No apparent decline of locomotor activity and no inhibition of liver transaminases were found. The compound appears to be safe for long-term use in Alzheimer's disease mouse model.

SUBMITTER: Lu J 

PROVIDER: S-EPMC4110911 | biostudies-literature | 2014 Aug

REPOSITORIES: biostudies-literature

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Syntheses, neural protective activities, and inhibition of glycogen synthase kinase-3β of substituted quinolines.

Lu Jianyu J   Maezawa Izumi I   Weerasekara Sahani S   Erenler Ramazan R   Nguyen Tuyen D T TD   Nguyen James J   Swisher Luxi Z LZ   Li Jun J   Jin Lee-Way LW   Ranjan Alok A   Srivastava Sanjay K SK   Hua Duy H DH  

Bioorganic & medicinal chemistry letters 20140604 15

A new series of fifteen 5-, 6-, and 8-appended 4-methylquinolines were synthesized and evaluated for their neural protective activities. Selected compounds were further examined for their inhibition of glycogen synthase kinase-3β (GSK-3β) and protein kinase C (PKC). Two most potent analogs, compounds 3 and 10, show nanomolar protective activities in amyloid β-induced MC65 cells and enzymatic inhibitory activities against GSK-3β, but poor PKC inhibitory activities. Using normal mouse model, the d  ...[more]

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