Browsing by Author "Saini, Vijayinder"

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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