PRATAP SHIVAJI DABHADE

@hrpatelpharmacy.co.in

Assistant Professor
H. R. Patel Institute of Pharmaceutical Education and Research

PRATAP SHIVAJI DABHADE


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https://researchid.co/pratap.dabhade

RESEARCH, TEACHING, or OTHER INTERESTS

Pharmacy, Chemistry, Cancer Research, Drug Discovery
8

Scopus Publications

105

Scholar Citations

6

Scholar h-index

4

Scholar i10-index

Scopus Publications

  • Design, Synthesis, and Biological Evaluation of Aminophenol–Quinazoline-Based Derivatives as Antiproliferative Agents Against Colorectal Cancer
    Sachin A. Dhawale, Pratap S. Dabhade, Santosh N. Mokale
    Chemistry and Biodiversity, 2026
    Quinazoline‐based scaffolds are well recognized for their therapeutic potential, particularly in the development of anticancer agents targeting tyrosine kinase‐mediated signaling pathways. In the present study, a series of novel quinazoline derivatives bearing cyclopropane‐1,1‐dicarboxamide moieties were designed, synthesized, and evaluated for their anticancer activity against human colorectal cancer (CRC) cell lines. The synthesized compounds were structurally characterized using 1H and 13C NMR spectroscopy and high‐resolution mass spectrometry. Their in vitro antiproliferative activity was assessed against HT‐29 and COLO‐205 cell lines using the MTT assay, with cabozantinib serving as the reference standard. Several compounds demonstrated promising cytotoxic activity, with compound SQ14 exhibiting the most potent inhibitory effect, comparable to the standard drug. Molecular docking and molecular dynamics simulations were performed to elucidate binding interactions and stability within the active site of the target protein, revealing favorable binding orientations and key intermolecular interactions. Furthermore, in silico ADMET analysis supported the drug‐like nature and acceptable pharmacokinetic profiles of the lead compounds. Overall, the integrated experimental and computational findings suggest that the newly synthesized quinazoline derivatives, particularly SQ14, represent promising candidates for further development as potential anticancer agents against CRC.
  • Microscale Synthesis, Characterization, and Anticancer Evaluation of Some ((E)-N-((2-(4-(1H-Imidazol-1-yl) Phenyl)-1H-Indol-3-yl) Methylene) Pyridin-2-Amine Derivatives
    Asian Journal of Green Chemistry, 2025
  • Diaryl Pyrazole-Chalcone Hybrids as Novel ER-α Modulators: Docking, Synthesis and Anti-Breast Cancer Activity Evaluation
    Advanced Journal of Chemistry Section A, 2025
  • Discovery of Novel Pyrimidine Based Small Molecule Inhibitors as VEGFR-2 Inhibitors: Design, Synthesis, and Anti-cancer Studies
    Sachin A. Dhawale, Santosh N. Mokale, Pratap S. Dabhade
    Current Computer Aided Drug Design, 2025
    Background: Receptor tyrosine kinases (RTKs) are potent oncoproteins in cancer that, when mutated or overexpressed, can cause uncontrolled growth of cells, angiogenesis, and metastasis, making them significant targets for cancer treatment. Vascular endothelial growth factor receptor 2 (VEGFR2), is a tyrosine kinase receptor that is produced in endothelial cells and is the most crucial regulator of angiogenic factors involved in tumor angiogenesis. So, a series of new substituted N-(4-((2-aminopyrimidin-5-yl)oxy)phenyl)-N-phenyl cyclopropane- 1,1-dicarboxamide derivatives as VEGFR-2 inhibitors have been designed and synthesized. Background: Receptor tyrosine kinases (RTKs) are potent oncoproteins in cancer that, when mutated or overexpressed, can cause uncontrolled growth of cells, angiogenesis, and metastasis, making them significant targets for cancer treatment. Vascular endothelial growth factor receptor 2 (VEGFR2), is a tyrosine kinase receptor that is produced in endothelial cells and is the most crucial regulator of angiogenic factors involved in tumor angiogenesis. So, a series of new substituted N-(4-((2-aminopyrimidin-5-yl)oxy)phenyl)-N-phenyl cyclopropane1,1-dicarboxamide derivatives as VEGFR-2 inhibitors have been designed and synthesized. Methods: Utilizing H-NMR, C13-NMR, and mass spectroscopy, the proposed derivatives were produced and assessed. HT-29 and COLO-205 cell lines were used for the cytotoxicity tests. The effective compound was investigated further for the Vegfr-2 kinase inhibition assay, cell cycle arrest, and apoptosis. A molecular docking examination was also carried out with the Maestro-12.5v of Schrodinger. Results: In comparison to the reference drug Cabozantinib (IC50 = 9.10 and 10.66 μM), compound SP2 revealed promising cytotoxic activity (IC50 = 4.07 and 4.98 μM) against HT-29 and COLO-205, respectively. The synthesized compound SP2 showed VEGFR-2 kinase inhibition activity with (IC50 = 6.82 μM) against the reference drug, Cabozantinib (IC50 = 0.045 μM). Moreover, compound SP2 strongly induced apoptosis by arresting the cell cycle in the G1 phase. The new compounds' potent VEGFR-2 inhibitory effect was noted with key amino acids Asp1044, and Glu883, and the hydrophobic interaction was also observed in the pocket of the VEGFR-2 active site by using a docking study. Conclusion: The results demonstrate that at the cellular and enzyme levels, the synthetic compounds SP2 are similarly effective as cabozantinib. The cell cycle and apoptosis data demonstrate the effectiveness of the suggested compounds. Based on the findings of docking studies, cytotoxic effects, in vitro VEGFR-2 inhibition, apoptosis, and cell cycle arrest, this research has given us identical or more effective VEGFR-2 inhibitors.
  • Design, Synthesis, Biological Evaluation and Molecular Modeling Studies of New Aminopyrimidine Derivatives as Potential Anticancer Agents
    Sachin A. Dhawale, Santosh N. Mokale, Pratap S. Dabhade
    Journal of Computational Biophysics and Chemistry, 2024
    A wide range of bioactive compounds have been created using the versatile pharmacophore pyrimidine. In order to improve biological applications, we, therefore, envisioned adding these privileged moieties. In this work, we developed an efficient 2-aminopyrimidine derivatives. We further investigated the anticancer activity of all the compounds against colon cancer cell lines COLO-205 and HT-29. Out of several compounds synthesized, two compounds SD2 and SD4 have shown comparable potent anticancer activity when compared to standard Cabozantinib. The most potent cytotoxic compound against colon cancer cells in our study was found to be SD2 with an IC50 value of 9.57 [Formula: see text]M. The investigation from molecular docking showed the best binding affinity. The complex stability within an enzyme’s pocket was demonstrated by the molecular dynamic simulation running for 100 ns.
  • Novel Pyrazole-Chalcone Hybrids: Synthesis and Computational Insights Against Breast Cancer
    Pratap S. Dabhade, Manjushri P. Dabhade, Lala S. Rathod, Sachin A. Dhawale, Shweta A. More, Somdatta Y. Chaudhari, Santosh N. Mokale
    Chemistry and Biodiversity, 2024
    More women die of breast cancer than of any other malignancy. The resistance and toxicity of traditional hormone therapy created an urgent need for potential molecules for treating breast cancer effectively. Novel biphenyl‐substituted pyrazole chalcones linked to a pyrrolidine ring were designed by using a hybridization approach. The hybrids were assessed against MCF‐7 and MDA‐MB‐231 cells by NRU assay. Among them, 8 k, 8 d, 8 m, 8 h, and 8 f showed significantly potent IC50 values: 0.17, 5.48, 8.13, 20.51, and 23.61 μM) respectively, on MCF‐7 cells compared to the positive control Raloxifene and Tamoxifen. Furthermore, most active compound 8 k [3‐(3‐(4‐fluorophenyl)‐1‐phenyl‐1H‐pyrazol‐4‐yl)‐1‐(2‐(2‐(pyrrolidin‐1‐yl)‐ethoxy)‐phenyl)‐chalcone] showed cell death induced through apoptosis, cell cycle arrest at the G2/M phase, and demonstrated decrease of ER‐α protein in western blotting study. Docking studies of 8 k and 8 d established adequate interactions with estrogen receptor‐α as required for SERM binding. The active hybrids exhibited good pharmacokinetic properties for oral bioavailability and drug‐likeness. Whereas, RMSD, RMSF, and Rg values from Molecular dynamics studies stipulated stability of the complex formed between compound 8 k and receptor. All of these findings strongly indicate the antiproliferative potential of pyrazole‐chalcone hybrids for the treatment of breast cancer.
  • Recent progress in targeting KRAS mutant cancers with covalent G12C-specific inhibitors
    Lala S. Rathod, Pratap S. Dabhade, Santosh N. Mokale
    Drug Discovery Today, 2023
  • Discovery of New Quinazoline Derivatives as VEGFR-2 Inhibitors: Design, Synthesis, and Anti-proliferative Studies
    Sachin A. Dhawale, Pratap S. Dabhade, Santosh N. Mokale
    Anti Cancer Agents in Medicinal Chemistry, 2023
    Background: In cancer, Receptor tyrosine kinases (RTKs) are powerful oncoproteins that can lead to uncontrolled cell proliferation, angiogenesis, and metastasis when mutated or overexpressed, making them crucial targets for cancer treatment. In endothelial cells, one of them is vascular endothelial growth factor receptor 2 (VEGFR2), a tyrosine kinase receptor that is produced and is the most essential regulator of angiogenic factors involved in tumor angiogenesis. So, a series of new N-(4-(4-amino-6,7-dimethoxyquinazolin-2-yloxy)phenyl)-N-phenyl cyclopropane-1,1- dicarboxamide derivatives as VEGFR-2 inhibitors have been designed and synthesized. Methods: The designed derivatives were synthesized and evaluated using H-NMR, C13-NMR, and Mass spectroscopy. The cytotoxicity was done with HT-29 and COLO-205 cell lines. The potent compound was further studied for Vegfr- 2 kinase inhibition assay. Furthermore, the highest activity compound was tested for cell cycle arrest and apoptosis. The molecular docking investigation was also done with the help of the Glide-7.6 program interfaced with Maestro- 11.3 of Schrodinger 2017. The molecular dynamics simulation was performed on the Desmond module of Schrodinger. Results: Compound SQ2 was observed to have promising cytotoxic activity (IC50 = 3.38 and 10.55 μM) in comparison to the reference drug Cabozantinib (IC50 = 9.10 and 10.66 μM) against HT-29 and COLO-205, respectively. The synthesized compound SQ2 showed VEGFR-2 kinase inhibition activity (IC50 = 0.014 μM) compared to the reference drug, Cabozantinib (IC50 = 0.0045 μM). Moreover, compound SQ2 strongly induced apoptosis by arresting the cell cycle in the G1 and G2/M phases. The docking study was performed to understand the binding pattern of the new compounds to the VEGFR-2 active site. Docking results attributed the potent VEGFR-2 inhibitory effect of the new compounds as they bound to the key amino acids in the active site, Asp1044, and Glu883, as well as their hydrophobic interaction with the receptor's hydrophobic pocket. The advanced computational study was also done with the help of molecular dynamics simulation. Conclusion: The findings show that the developed derivatives SQ2 and SQ4 are equally powerful as cabozantinib at cellular and enzymatic levels. The apoptosis and cell cycle results show that the proposed compounds are potent. This research has provided us with identical or more potent VEGFR-2 inhibitors supported by the results of docking studies, molecular dynamics simulation, cytotoxic actions, in vitro VEGFR-2 inhibition, apoptosis, and cell cycle arrest.

RECENT SCHOLAR PUBLICATIONS

  • Design, Synthesis, and Biological Evaluation of Aminophenol–Quinazoline‐Based Derivatives as Antiproliferative Agents Against Colorectal Cancer
    SA Dhawale, PS Dabhade, SN Mokale
    Chemistry & Biodiversity 23 (3), e02491 , 2026
    2026
  • Discovery of novel pyrimidine based small molecule inhibitors as VEGFR-2 inhibitors: design, synthesis, and anti-cancer studies
    SA Dhawale, SN Mokale, PS Dabhade
    Current Computer-Aided Drug Design 21 (1), 38-49 , 2025
    2025
    Citations: 2
  • Microscale Synthesis, Characterization, and Anticancer Evaluation of Some ((E)-N-((2-(4-(1H-Imidazol-1-yl) Phenyl)-1HIndol-3-yl) Methylene) Pyridin-2-Amine Derivatives
    MP Dabhade, PS Dabhade, GS Talele
    Asian Journal of Green Chemistry 9 (3), 310-328 , 2025
    2025
  • Asian Journal of Green Chemistry
    MP Dabhade, PS Dabhade, GS Talele
    2025
  • Comprehensive In Silico Screening of Some Indole Derivatives as Potential Selective Oestrogen Receptor Degrader (SERD)
    MP Dabhade, PS Dabhade, GS Talele
    2025
  • Diaryl Pyrazole-Chalcone Hybrids as Novel ER-α Modulators: Docking, Synthesis and Anti-Breast Cancer Activity Evaluation
    SNM Pratap S Dabhade, Manjushri P Dabhade, Sachin A Dhawale, Lala S Rathod
    Advanced Journal of Chemistry, Section A 8 (2), 341-360 , 2024
    2024
    Citations: 8
  • Design, synthesis, biological evaluation, and molecular modeling studies of new aminopyrimidine derivatives as potential anticancer agents
    SA Dhawale, SN Mokale, PS Dabhade
    Journal of Computational Biophysics and Chemistry , 2024
    2024
  • Ultrasonic and Microwave Accelerated Vilsmeier-Haack Formylation: An Energy-efficient Route to Synthesize Pyrazole-4-Carbaldehydes.
    PS Dabhade, MP Dabhade, SA Dhawale, SN Mokale
    Degrés 9 (7), 85-99 , 2024
    2024
  • Novel pyrazole‐chalcone hybrids: synthesis and computational insights against breast cancer
    PS Dabhade, MP Dabhade, LS Rathod, SA Dhawale, SA More, ...
    Chemistry & Biodiversity 21 (7), e202400015 , 2024
    2024
    Citations: 11
  • Discovery of new quinazoline derivatives as VEGFR-2 inhibitors: Design, synthesis, and anti-proliferative studies
    SA Dhawale, PS Dabhade, SN Mokale
    Anti-Cancer Agents in Medicinal Chemistry-Anti-Cancer Agents) 23 (18), 2042-2055 , 2023
    2023
    Citations: 7
  • A NOVEL PYRAZOLECHALCONES HAVING ANTI-CANCER ACTIVITY
    MPD Pratap S.Dabhade, Santosh N. Mokale
    IN Patent 06/2,023 , 2023
    2023
  • Recent progress in targeting KRAS mutant cancers with covalent G12C-specific inhibitors
    SNM Lala S. Rathod, Pratap S. Dabhade
    Drug Discovery Today, 103557 , 2023
    2023
    Citations: 34
  • Synthesis, Pharmacological Screening and Docking Analysis of Some Novel Pyrazole Chalchones as Anti-Cancer Agents
    P Dabhade, DSN Mokale, M Dabhade
    Proceedings of International Conference on Drug Discovery (ICDD) , 2020
    2020
  • Analytical method development and validation for determination of Nimorazole in bulk and dosage form by RP-HPLC
    Dabhade, P., S., Ghorpade, H., S.
    Asian Journal of Pharmaceutical Analysis and Medicinal Chemistry 5 (2), 73-78 , 2017
    2017
  • RP-HPLC method development and validation of azelnidipine
    MG Gore, PS Dabhade
    International Journal of Pharmaceutical Sciences and Research 7 (12), 5111 , 2016
    2016
    Citations: 20
  • An Herbal PH Indicator from Bracts Extract of Bougainvillea Spectabilis
    Dabhade, P., S., Bagul, S., B.
    Pharmagene 2 (3) , 2016
    2016
  • Solubility and dissolution enhancement of gliclazide by solid dispersion technique
    CG More, PS Dabhade, NP Jain, BO Aher
    International Journal of Pharmaceutical Chemistry and Analysis 2 (2), 51-58 , 2015
    2015
    Citations: 14
  • Synthesis and Evaluation of 2, 4, 5-Trisubstituted and 1, 2, 4, 5 Tetrasubstituted Imidazole as Antimicrobial Agents
    MG Kanawade, PS Dabhade, AS Dange
    Journal of Current Pharma Research 3 (4), 989 , 2013
    2013
    Citations: 1
  • Synthesis and evaluation of antifungal activity of benzotriazole derivatives.
    PS Dabhade
    2013
    Citations: 4
  • Microwave Assisted Synthesis and Evaluation of Some Substituded Novel Thiazole as Antimicrobial Agents
    Dabhade, P., S., Dange, A., S.
    International Journal of Universal Pharmacy and Life Sciences 3 (6), 207-214 , 2013
    2013

MOST CITED SCHOLAR PUBLICATIONS

  • Recent progress in targeting KRAS mutant cancers with covalent G12C-specific inhibitors
    SNM Lala S. Rathod, Pratap S. Dabhade
    Drug Discovery Today, 103557 , 2023
    2023
    Citations: 34
  • RP-HPLC method development and validation of azelnidipine
    MG Gore, PS Dabhade
    International Journal of Pharmaceutical Sciences and Research 7 (12), 5111 , 2016
    2016
    Citations: 20
  • Solubility and dissolution enhancement of gliclazide by solid dispersion technique
    CG More, PS Dabhade, NP Jain, BO Aher
    International Journal of Pharmaceutical Chemistry and Analysis 2 (2), 51-58 , 2015
    2015
    Citations: 14
  • Novel pyrazole‐chalcone hybrids: synthesis and computational insights against breast cancer
    PS Dabhade, MP Dabhade, LS Rathod, SA Dhawale, SA More, ...
    Chemistry & Biodiversity 21 (7), e202400015 , 2024
    2024
    Citations: 11
  • Diaryl Pyrazole-Chalcone Hybrids as Novel ER-α Modulators: Docking, Synthesis and Anti-Breast Cancer Activity Evaluation
    SNM Pratap S Dabhade, Manjushri P Dabhade, Sachin A Dhawale, Lala S Rathod
    Advanced Journal of Chemistry, Section A 8 (2), 341-360 , 2024
    2024
    Citations: 8
  • Discovery of new quinazoline derivatives as VEGFR-2 inhibitors: Design, synthesis, and anti-proliferative studies
    SA Dhawale, PS Dabhade, SN Mokale
    Anti-Cancer Agents in Medicinal Chemistry-Anti-Cancer Agents) 23 (18), 2042-2055 , 2023
    2023
    Citations: 7
  • Synthesis and evaluation of antifungal activity of benzotriazole derivatives.
    PS Dabhade
    2013
    Citations: 4
  • A herbal pH indicator from bracts extract of Bougainvillea spectabilis
    SB Bagul, MP Dabhade, P Dabhade, TD Bhamare
    A Genes J Pharmagene 2, 11-3 , 2012
    2012
    Citations: 4
  • Discovery of novel pyrimidine based small molecule inhibitors as VEGFR-2 inhibitors: design, synthesis, and anti-cancer studies
    SA Dhawale, SN Mokale, PS Dabhade
    Current Computer-Aided Drug Design 21 (1), 38-49 , 2025
    2025
    Citations: 2
  • Synthesis and Evaluation of 2, 4, 5-Trisubstituted and 1, 2, 4, 5 Tetrasubstituted Imidazole as Antimicrobial Agents
    MG Kanawade, PS Dabhade, AS Dange
    Journal of Current Pharma Research 3 (4), 989 , 2013
    2013
    Citations: 1
  • Design, Synthesis, and Biological Evaluation of Aminophenol–Quinazoline‐Based Derivatives as Antiproliferative Agents Against Colorectal Cancer
    SA Dhawale, PS Dabhade, SN Mokale
    Chemistry & Biodiversity 23 (3), e02491 , 2026
    2026
  • Microscale Synthesis, Characterization, and Anticancer Evaluation of Some ((E)-N-((2-(4-(1H-Imidazol-1-yl) Phenyl)-1HIndol-3-yl) Methylene) Pyridin-2-Amine Derivatives
    MP Dabhade, PS Dabhade, GS Talele
    Asian Journal of Green Chemistry 9 (3), 310-328 , 2025
    2025
  • Asian Journal of Green Chemistry
    MP Dabhade, PS Dabhade, GS Talele
    2025
  • Comprehensive In Silico Screening of Some Indole Derivatives as Potential Selective Oestrogen Receptor Degrader (SERD)
    MP Dabhade, PS Dabhade, GS Talele
    2025
  • Design, synthesis, biological evaluation, and molecular modeling studies of new aminopyrimidine derivatives as potential anticancer agents
    SA Dhawale, SN Mokale, PS Dabhade
    Journal of Computational Biophysics and Chemistry , 2024
    2024
  • Ultrasonic and Microwave Accelerated Vilsmeier-Haack Formylation: An Energy-efficient Route to Synthesize Pyrazole-4-Carbaldehydes.
    PS Dabhade, MP Dabhade, SA Dhawale, SN Mokale
    Degrés 9 (7), 85-99 , 2024
    2024
  • A NOVEL PYRAZOLECHALCONES HAVING ANTI-CANCER ACTIVITY
    MPD Pratap S.Dabhade, Santosh N. Mokale
    IN Patent 06/2,023 , 2023
    2023
  • Synthesis, Pharmacological Screening and Docking Analysis of Some Novel Pyrazole Chalchones as Anti-Cancer Agents
    P Dabhade, DSN Mokale, M Dabhade
    Proceedings of International Conference on Drug Discovery (ICDD) , 2020
    2020
  • Analytical method development and validation for determination of Nimorazole in bulk and dosage form by RP-HPLC
    Dabhade, P., S., Ghorpade, H., S.
    Asian Journal of Pharmaceutical Analysis and Medicinal Chemistry 5 (2), 73-78 , 2017
    2017
  • An Herbal PH Indicator from Bracts Extract of Bougainvillea Spectabilis
    Dabhade, P., S., Bagul, S., B.
    Pharmagene 2 (3) , 2016
    2016