Novel carbocyclic nucleoside analogs suppress glomerular mesangial cells proliferation and matrix protein accumulation through ROS-dependent mechanism in the diabetic milieu. II. Acylhydrazone-functionalized pyrimidines

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• 作者：Kamal H. Bouhadir^a ; ^{kb05@aub.edu.lb" class="auth_mail" title="E-mail the corresponding author} ; Ali Koubeissi^a ; ^&dagger ; ; Fatima A. Mohsen^b ; ^&dagger ; ; Mira Diab El-Harakeh^a ; Rouba Cheaib^a ; Joan Younes^c ; Georges Azzi^d ; Assaad A. Eid^b ; ^{ae49@aub.edu.lb" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Carbocyclic nucleosides ; Acylhydrazones ; Diabetic nephropathy ; Uracil ; Thymine ; Cytosine
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 February 2016
• 年：2016
• 卷：26
• 期：3
• 页码：1020-1024
• 全文大小：820 K

文摘

We report herein the synthesis of a novel series of carbocyclic acylhydrazone derivatives of uracil, thymine and cytosine from the corresponding nucleic bases and their biological activity to treat diabetic nephropathy. Intriguingly, five derivatives significantly reduced high-glucose induced glomerular mesangial cells proliferation and matrix protein accumulation in vitro. The anti-oxidative effects displayed by these molecules suggest that their activity might involve a ROS-dependent mechanism.