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Publications

Publications on kinase inhibitor drug discovery

Research papers:​

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  • Wadje BN, Somarowthu T, Thakur S, Jadhav HR, Bharate SB.* Structure-Based Virtual Screening of FDA-approved Drugs to Discover Potential Inhibitors of Phosphoinositide Kinase, PIKfyveJ. Biomol. Struct. Dyn. 2024, In Press.

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  • Bhurta D, Hossain MM, Bhardwaj M, Showket F, Nandi U, Dar MJ, Bharate SB* Orally Bioavailable Styryl Derivative of Rohitukine-N-oxide Inhibits CDK9/T1 and the Growth of Pancreatic Cancer cells. Eur. J. Med. Chem. 2023, 258, 115533

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  • Bhurta D, Bharate SB* Discovery of Pongol, the Furanoflavonoid, as an Inhibitor of CDK7/Cyclin H/MAT1, and its Preliminary Structure-Activity Relationship. ACS Omega, 2023, 8 (1), 1291–1300

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  • Bharate SB;* Kumar V; Jain SK; Mintoo NJ; Guru SK; Nuthakki VK; Sharma M; Bharate SS; Gandhi SG; Mondhe DM; Bhushan S; Vishwakarma RA. Discovery and Preclinical Development of IIIM-290, an Orally Active Potent Cyclin-dependent Kinase Inhibitor. J. Med. Chem. 2018, 61, 1664-1687

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  • Joshi P; Gupta M; Vishwakarma RA; Kumar A; Bharate SB* (Z)-2-(3-Chlorobenzylidene)-3,4-dihydro-N-(2-methoxyethyl)-3-oxo-2H-benzo[b][1,4]oxazine-6-carboxamide as GSK-3beta inhibitor: Identification by virtual screening, and its validation in enzyme and cell-based assay. Chem. Biol. Drug. Des., 2017, 89, 964−971.

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  • Kumar V; Guru SK; Jain SK; Joshi P; Gandhi SG; Bharate SB; Bhushan S; Bharate SS; Vishwakarma RA. A chromatography-free isolation of rohitukine from leaves of Dysoxylum binectariferum: Evaluation for in vitro cytotoxicity, Cdk inhibition and physicochemical properties. Bioorg. Med. Chem. Lett., 2016, 26, 3457-3463

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  • Yadav RR; Guru SK; Joshi P; Mahajan G; Mintoo MJ; Kumar V; Bharate SS; Mondhe DM; Vishwakarma RA; Bhushan S; Bharate SB* 6-Aryl substituted 4-(4-cyanomethyl) phenylamino quinazolines as a new class of isoform-selective PI3K-alpha inhibitors. Eur. J. Med. Chem., 2016, 122, 731-743

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Key Reviews/ Perspectives:

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  • Bhurta D, Bharate SB.* Analyzing the Scaffold Diversity of Cyclin-dependent Kinase Inhibitors and Revisiting the Clinical and Preclinical Pipeline. Med. Res. Rev. 2022, 42, 2, 654-709.

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  • Bharate SB;* Yadav RR; Battula S; Vishwakarma RA. Meridianins: A potent marine derived kinase inhibitors. Mini-Rev. Med. Chem., 2012, 12 (7), 618-631.

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  • Jain SK; Bharate SB;* Vishwakarma RA.  Cyclin-dependent kinase inhibition by flavoalkaloids. Mini-Rev. Med. Chem., 2012, 12 (7), 632-649.

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  • Bharate SB;* Manda S; Mupparapu N; Battini N; Vishwakarma RA. Chemistry and biology of fascaplysin, a potent marine-derived CDK-4 inhibitor. Mini-Rev. Med. Chem., 2012, 12 (7), 650-664.

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Patents:

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  • Fused pyrimidines as isoform-selective phosphoinositide-3-kinase-alpha inhibitors and process for preparation thereof. WO2017090058A1.

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  • Rohitukine analogs as cyclin-dependent kinase inhibitors and a process for the preparation thereof. WO2014170914A1.

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  • 6-Aryl-4-phenylamino-quinazoline analogs as phosphoinositide-3-kinase inhibitors. WO2015128873A1.

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  • Solid dispersion comprising and anticancer compound with improved solubility and efficacy. WO202012498A1.

For Detailed List of Publications, Please visit:

 

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