School Of Health Sciences

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Author: search.filters.author.Kumar, Vinod

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    Design, synthesis, and biological evaluation of N-[1-(6?-chloropyridazin-3?-yl)-3-(4?-substitutedphenyl)-1H-pyrazole-5-yl]alkanamides as anti-inflammatory agents
    (John Wiley and Sons Inc, 2022-01-22T00:00:00) Aggarwal, Ranjana; Swati, S.; Kumar, Vinod; Singh, Randhir; Kajal, Anu; Saini, Deepika
    A series of structurally diverse N-[1-(6?-chloropyridazin-3?-yl)-3-(4?-substitutedphenyl)-1H-pyrazole-5-yl]alkanamides 5(a�r) has been designed and synthesized via Aliquat 336 catalyzed amidation of 5-amino-3-aryl-1-(6?-chloropyridazin-3?-yl)pyrazoles 3(a�c). The target compounds were designed on basis of the results obtained from the study of Lipinski's rule of five and binding interactions with target protein 3LN1. Eventually, compounds 5(a�r) were screened for their in vitro anti-inflammatory action by using inhibition of albumin denaturation and membrane stabilization assay. It has been found that all the synthesized compounds obeyed Lipinski's rule of five (nviolations�=�0�1) and showed weak to strong binding interactions with dock score range ?8.0 to ?9.9�kcal/mol. All alkanamides exhibited moderate to excellent activity as compared to the standard drug, Aspirin. Interestingly, the results indicated that the compound 5a may act as a promising medicinal lead as an anti-inflammatory agent for in vivo and clinical testing in future. � 2022 Wiley Periodicals LLC.
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    Recent updates on the therapeutic potential of HER2 tyrosine kinase inhibitors for the treatment of breast cancer
    (Bentham Science Publishers B.V., 2018) Singla, Heena; Munshi, Anjana; Banipal, Raja Paramjit Singh; Kumar, Vinod
    HER2 positive breast cancer is characterized by the low survival rate in the metastatic patients. Development of resistance and disease-relapse are the major problems associated with the currently available therapies for HER2 positive breast cancer. There are two major targeted therapies for HER2 positive breast cancer viz. monoclonal antibodies and tyrosine-kinase inhibitors, and both of these therapies have their advantages and limitations. To address the limitations associated with the existing therapies, use of antibodies and TKIs as combination therapy proved to be more effective. Various chemical modifications can be performed on tyrosine-kinase inhibitors to develop novel ligands with increased selectivity for HER2 kinase. A number of tyrosine-kinase inhibitors are in various phases of clinical trials for the treatment of HER2 positive breast cancer. In the current review article, recent developments on various HER2 tyrosine-kinase inhibitors have been reported. Various structurally different scaffolds bind to the HER2 receptor and exhibit potent anti-cancer activities. The structural and pharmacophoric requirements of the scaffolds are discussed in detail so as to discover effective drug candidates for the treatment of HER2 positive breast cancer. ? 2018 Bentham Science Publishers.
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    Recent advances in HER2 positive breast cancer epigenetics: Susceptibility and therapeutic strategies
    (Elsevier Masson SAS, 2017) Singla, Heena; Ludhiadch, Abhilash; Kaur, Raman Preet; Chander, Harish; Kumar, Vinod; Munshi, Anjana
    HER2 amplification/overexpression accounts for aggressive clinical features of HER2 positive breast cancer. Epigenetic changes including DNA methylation, histone modifications and ncRNAs/miRNAs are associated with regulation of DNA chromatin and specifically, gene transcription. Hence, these produce eminent effects upon proto-oncogenes, tumor-suppressors and key cancer-regulatory signaling pathways. Understanding of epigenomic regulation of HER2 overexpression and signaling may help uncover the unmatchable physiology of HER2 gene/protein. Moreover, this may also aid in resolving the major issue of resistance-development towards HER2 targeted agents (trastuzumab and lapatinib), since epigenetic alterations are important therapeutic markers and modulate the response towards HER2 targeted therapy. Therefore, in this review the information regarding various epigenetic markers implicated in HER2 positive breast cancer susceptibility and therapeutic-strategies has been compiled. ? 2017 Elsevier Masson SAS