Publications

Publications on kinase inhibitor drug discovery

Research papers:

Raghuvanshi R, Wakudkar SC, Manda S, Bharate SB. Design, synthesis, and biological evaluation of kenpaullone derivatives as potential dual inhibitors of cholinesterases and glycogen synthase kinase-3β. Bioorg. Chem. 2025, 167, 109232

Mohammed S, Thakur S, Manhas D, Reddy CN, Eedara A, Guru SK, Singh A, Bhardwaj M, Kambhampati V, Pandian R, Gopu B, Bhushan S, Vishwakarma RA, Andugulapati SB, Singh SK, Nandi U, Bharate SB.* Discovery of 2-(4-Ureido-piperidin-1-yl)-4-morpholinothieno [3,2-d] pyrimidines as Orally Bioavailable Phosphoinositide-3-kinase Inhibitors with In Vitro and In Vivo Antitumor Efficacy in Triple-Negative Breast Cancer. J. Med. Chem., 2025, 68 (20), 21282–21317

Nayak M, Kallurkar KV, Somrowthu T, Nanubolu JB, Bharate SB. Total Synthesis of Rohitukine and Dysoline and Their Anticancer Analogues Flavopiridol and IIIM-290. ACS Omega, 2025, 10, 38240−38254

Somarowthu T, Patekar RR, Bharate SB.* Identification of Mitoxantrone as a Potent Inhibitor of CDK7/Cyclin H via Structure-Based Virtual Screening and In-Vitro Validation by ADP-Glo Kinase Assay. Bioorg. Chem. 2025, 155, 108111

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

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

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

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.

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

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

Yadav RR; Sharma S; Joshi P; Wani A; Vishwakarma RA; Kumar A; Bharate SB* Meridianin derivatives as potent Dyrk1A inhibitors and neuroprotective agents. Bioorg. Med. Chem. Lett. 2015, 25, 2948-295

Key Reviews/ Perspectives:

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.

Raghuvanshi R.; Bharate SB.* Recent developments in the use of kinase inhibitors in management of viral infections. J. Med. Chem. 2022, 65, 2, 893-921.

Raghuvanshi R; Bharate SB* Preclinical and clinical studies on bryostatins, a class of marine-derived protein kinase C modulators: A mini-review. Curr. Topics Med. Chem. 2020, 20 (12), 1124-1135.

Bharate SB; Sawant SD; Singh PP; Vishwakarma RA. Kinase inhibitors of marine origin. Chem. Rev., 2013, 113, 6761-6815.

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

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

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.

Patents:

2-Aminopyrimido[4',5':3,4] cyclohepta[1,2-b]indoles as anti-SARS-CoV-2 agents and process for preparation thereof. IN 202511018217.
Solid dispersion comprising and anticancer compound with improved solubility and efficacy. WO202012498A1.

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

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

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