Pharmaceutical Sciences and Natural Products - Master Dissertation

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http://10.2.3.109/handle/32116/53

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Browsing Pharmaceutical Sciences and Natural Products - Master Dissertation by Author "Kumar, Vinod"

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    3-D QSAR Study Of Combretastatins Fused With Hetrocyclic Ring As Tubulin Binding Agents
    (Central University of Punjab, 2018) Dhanka, Ajit Kumar; Kumar, Vinod
    Combretastatin A4 (CA4) is a leading agent in vascular disrupting strategies and tubulin polymerization inhibitor for the tumour therapy. A large number of combretastatin derivatives have been synthesized as potent inhibitors of Tubulin which are responsible for the anticancer activity. Combretastatins bind with the colchicine binding site of the tubulin and disrupt the dynamic equilibrium of tubulin. IN the current research proposal we have performed 3D-Field based QSAR on Combretastatins analogue in order to recognize structural features which are responsible for the tubulin inhibitors activity. The designed compounds are expected to show good inhibitory activity against tubulin when electrostatic group is attached in case of compounds 16 and 18, Bulky group is attached in case of compound 26 and hydrophobic group is attached in case of compound 51 respectively.
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    Design and synethesis of putative anti-cancer agents using hybrid molecular approach
    (Central University of Punjab, 2014) Saini, Vijayinder; Kumar, Vinod
    A Hybrid drug involves the unification of two drug pharmacophores in one single molecule. The hybrid drugs are designed to interact with multiple targets or to intensify its effect through action on another bio target as one single molecule or to counterbalance the known side effects associated with the other hybrid part. One of the important role of hybrid drugs is to counter multidrug resistance. Muti-drug resistance observed during the treatment for cancer. Target therapy for various cancer are developed and successfully used to treat cancer patient. But treatment can be further strengthen by concurrent administration of single drug by combining two different drugs from different origin act at different receptor to cope MDR. It is also said as to load a multi-target drug in a single drug. In the current research proposal, we have designed and synthesized molecules which affect tubulin polymerization as well as MetAP-2 receptor. Both play vital role in tumor progression by strengthening the cell cytoskeleton and angiogenesis process respectively. The hybrids of chalcone (antitubulin) and arylazole (anti MetAP-2) were synthesized and molecular docking studies were performed. The compounds were synthesized by three step reaction and synthesized compounds were analyzed and confirmed by FTIR, NMR and mass spectrometry. The activity of synthesized compound was evaluated against HCT-116 (wild & null type) colon cancer cell lines at a concentration of 5 μM, 25 μM and 50 μM. Compounds were equally active in wild type and null type HTC-116 cell lines with slight less inhibition in null type. Lastly, the information on inhibitory potential of compounds v were obtained from MTT assay wherein VJ-4, VJ-2PP2 & VJ-4PP1 were found to be active anticancer agents
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    Synthesis And Biological Evaluation Of Pyrimidine Bridged Biphenyls As Putative Ligands To Target Parkinson's Disease
    (Central University of Punjab, 2018) Bala, Manu; Kumar, Vinod
    MAO inhibitors have been explored as therapeutic agents for the treatment or management of PD. A series of 2,4,6-trisubstituted pyrimidine derivatives incorporating a propargyl moiety were synthesized and screened for their MAO inhibition potential using Amplex® Red assay. All the compounds showed good inhibitory activity for MAO-B. The structure-activity relationship profile has been developed with number of electron releasing and electron withdrawing substituents attached to the pyrimidine nucleus. MV7 was found to be the most potent MAO-B inhibitor with IC50 value of 0.44 ± 0.02 ?M. From molecular docking studies, it was found that compounds fit well in the active site of MAO-B isoform near FAD cofactor. Thus, the active compound MV7 obtained in this series can act as promising lead for the development of effective and potent MAO-B inhibitor for the treatment of Parkinson's disease.