Literature DB >> 18280153

Rational design of 4-amino-5,6-diaryl-furo[2,3-d]pyrimidines as potent glycogen synthase kinase-3 inhibitors.

Yasushi Miyazaki1, Yutaka Maeda, Hideyuki Sato, Masato Nakano, Geoffrey W Mellor.   

Abstract

4-Amino-5,6-diaryl-furo[2,3-d]pyrimidines have been identified as inhibitors of glycogen synthase kinase-3beta (GSK-3beta). One representative derivative, 4-amino-3-(4-(benzenesulfonylamino)-phenyl)-2-(3-pyridyl)-furo[2,3-d]pyrimidine (12) exhibited potent GSK-3beta inhibitory activity in low nanomolar level of IC(50). The binding mode was proposed from a docking study.

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Year:  2008        PMID： 18280153     DOI： 10.1016/j.bmcl.2008.01.113

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  10 in total

1.  Crystal structure and NMR binding reveal that two small molecule antagonists target the high affinity ephrin-binding channel of the EphA4 receptor.

Authors:  Haina Qin; Jiahai Shi; Roberta Noberini; Elena B Pasquale; Jianxing Song
Journal:  J Biol Chem       Date:  2008-08-14       Impact factor: 5.157

2.  Small molecules can selectively inhibit ephrin binding to the EphA4 and EphA2 receptors.

Authors:  Roberta Noberini; Mitchell Koolpe; Satyamaheshwar Peddibhotla; Russell Dahl; Ying Su; Nicholas D P Cosford; Gregory P Roth; Elena B Pasquale
Journal:  J Biol Chem       Date:  2008-08-26       Impact factor: 5.157

3.  Efficient one-pot synthesis of novel and diverse furo[2,3-d] pyrimidinediones and thioxofuro[2,3-d] pyrimidineones by the rhodium (II) pivalate-catalyzed reactions of cyclic diazo compounds.

Authors:  Krishna Bahadur Somai Magar; Yong Rok Lee; Sung Hong Kim
Journal:  Mol Divers       Date:  2013-08-02       Impact factor: 2.943

4.  Investigation of naphthofuran moiety as potential dual inhibitor against BACE-1 and GSK-3β: molecular dynamics simulations, binding energy, and network analysis to identify first-in-class dual inhibitors against Alzheimer's disease.

Authors:  Akhil Kumar; Gaurava Srivastava; Swati Srivastava; Seema Verma; Arvind S Negi; Ashok Sharma
Journal:  J Mol Model       Date:  2017-07-24       Impact factor: 1.810

Review 5.  Glycogen synthase kinase 3: more than a namesake.

Authors:  Geetha Vani Rayasam; Vamshi Krishna Tulasi; Reena Sodhi; Joseph Alex Davis; Abhijit Ray
Journal:  Br J Pharmacol       Date:  2009-03-04       Impact factor: 8.739

6.  Merging catalyst-free synthesis and iodine catalysis: one-pot synthesis of dihydrofuropyrimidines and spirodihydrofuropyrimidine pyrazolones.

Authors:  Ya-Yun Zheng; Kai-Xiang Feng; Ai-Bao Xia; Jie Liu; Cheng-Ke Tang; Zhan-Yu Zhou; Dan-Qian Xu
Journal:  RSC Adv       Date:  2019-03-27       Impact factor: 3.361

7.  Synthesis, biological evaluation and docking studies of 1,2,4-oxadiazole linked 5-fluorouracil derivatives as anticancer agents.

Authors:  Ravi Kumar Bommera; Shashikala Kethireddy; Rajeshwar Reddy Govindapur; Laxminarayana Eppakayala
Journal:  BMC Chem       Date:  2021-05-04

8.  An efficient diastereoselective synthesis of novel fused 5H-furo[2,3-d]thiazolo[3,2-a]pyrimidin-5-ones via one-pot three-component reaction.

Authors:  Tooba Tabibi; Abbas Ali Esmaeili; Joel T Mague
Journal:  Mol Divers       Date:  2021-01-03       Impact factor: 2.943

9.  Small-Molecule Inhibitors of GSK-3: Structural Insights and Their Application to Alzheimer's Disease Models.

Authors:  Thomas Kramer; Boris Schmidt; Fabio Lo Monte
Journal:  Int J Alzheimers Dis       Date:  2012-07-22

10.  Design, Synthesis, Molecular Modeling and Antitumor Evaluation of Novel Indolyl-Pyrimidine Derivatives with EGFR Inhibitory Activity.

Authors:  Naglaa M Ahmed; Mahmoud M Youns; Moustafa K Soltan; Ahmed M Said
Journal:  Molecules       Date:  2021-03-25       Impact factor: 4.411
  10 in total

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