Literature DB >> 12941335

Bone-targeted 2,6,9-trisubstituted purines: novel inhibitors of Src tyrosine kinase for the treatment of bone diseases.

Yihan Wang1, Chester A Metcalf, William C Shakespeare, Raji Sundaramoorthi, Terence P Keenan, Regine S Bohacek, Marie Rose van Schravendijk, Shiela M Violette, Surinder S Narula, David C Dalgarno, Chad Haraldson, Jeffrey Keats, Shuenn Liou, Ukti Mani, Selvi Pradeepan, Mary Ram, Susan Adams, Manfred Weigele, Tomi K Sawyer.   

Abstract

Novel bone-targeted 2,6,9-trisubstituted purine template-based inhibitors of Src tyrosine kinase are described. Drug design studies of known purine compounds revealed that both positions-2 and -6 were suitable for incorporating bone-seeking moieties. A variety of bone-targeting groups with different affinity to hydroxyapatite were utilized in the study. Compound 3d was determined to be a potent Src inhibitor and was quite selective against a panel of other protein kinases.

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Year:  2003        PMID: 12941335     DOI: 10.1016/s0960-894x(03)00648-6

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


  5 in total

1.  Discriminating of ATP competitive Src kinase inhibitors and decoys using self-organizing map and support vector machine.

Authors:  Aixia Yan; Xiaoying Hu; Kai Wang; Jing Sun
Journal:  Mol Divers       Date:  2012-11-02       Impact factor: 2.943

2.  Antiangiogenic and antitumor effects of SRC inhibition in ovarian carcinoma.

Authors:  Liz Y Han; Charles N Landen; Jose G Trevino; Jyotsnabaran Halder; Yvonne G Lin; Aparna A Kamat; Tae-Jin Kim; William M Merritt; Robert L Coleman; David M Gershenson; William C Shakespeare; Yihan Wang; Raji Sundaramoorth; Chester A Metcalf; David C Dalgarno; Tomi K Sawyer; Gary E Gallick; Anil K Sood
Journal:  Cancer Res       Date:  2006-09-01       Impact factor: 12.701

3.  Crystal Structures of the p21-activated kinases PAK4, PAK5, and PAK6 reveal catalytic domain plasticity of active group II PAKs.

Authors:  Jeyanthy Eswaran; Wen Hwa Lee; Judit E Debreczeni; Panagis Filippakopoulos; Andrew Turnbull; Oleg Fedorov; Sean W Deacon; Jeffrey R Peterson; Stefan Knapp
Journal:  Structure       Date:  2007-02       Impact factor: 5.006

Review 4.  New Progress in Improving the Delivery Methods of Bisphosphonates in the Treatment of Bone Tumors.

Authors:  Yu Zhong; Su Li
Journal:  Drug Des Devel Ther       Date:  2021-12-10       Impact factor: 4.162

5.  Promising 2,6,9-Trisubstituted Purine Derivatives for Anticancer Compounds: Synthesis, 3D-QSAR, and Preliminary Biological Assays.

Authors:  Cristian O Salas; Ana Maria Zarate; Vladimir Kryštof; Jaime Mella; Mario Faundez; Jose Brea; María Isabel Loza; Ivan Brito; Denisa Hendrychová; Radek Jorda; Alan R Cabrera; Ricardo A Tapia; Christian Espinosa-Bustos
Journal:  Int J Mol Sci       Date:  2019-12-25       Impact factor: 5.923

  5 in total

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