A series of novel phosphorylated derivatives of didanosine were designed and docking studies were performed with a fusion protein of the Newcastle disease virus (NDV), to develop antiviral compounds against NDV. Based on the docking scores and binding affinities, three derivatives were selected. These compounds were synthesized and characterized by IR, (1) H, (13) C, (31) P, and CHN analysis and mass spectra. They were assessed for their in vitro antiviral activity in DF-1 cells; DDI-10 showed better antiviral activity as evidenced by significant reduction in plaque formation and cytopathic effects. DDI-10 was further evaluated in NDV-infected chicken; the survival rates and antioxidant enzyme levels in brain, liver, and lung tissues were estimated. Superoxide dismutase and catalase were significantly raised, and lipid peroxidation and HA titer levels were decreased upon treatment with 1.5 mg/kg body weight of DDI-10 than with 3 mg/kg body weight of DDI. Further histopathological alterations in NDV-infected tissues were restored in chicken treated with DDI-10. Thus, based on the results from in silico, in vitro, and in vivo assays, the novel phosphorylated DDI-10 might be considered as potent antiviral compound for NDV infection in chicken.
Breast cancer has a rate of occurrence of one in nine. Aromatase also named estrogen synthase which is found to be associated with breast cancer and it has also been one of the targets for treatment and the current work explores the potentiality of a new heteroaryl a-aminophosphonates 9 a-j. The new heteroaryl a-aminophosphonates 9 a-j were synthesized using the reactions involving 2-aminobenzothiazole (6), various heteroaryl aldehydes 7 a-j and 2,3-dihydro[1, 3,2]oxazaphospholo[4, 5-b]pyridine-2-oxide (5). The QSAR (quantitative structure activity relationship) descriptors, PreADMET (adsorption, distribution, metabolism, excretion and toxicity) analysis and binding interaction simulation studies with X-Ray crystallographic structure of Aromatase have positively forwarded us for the cytotoxicity evaluation of the title compounds by Morphological study, Cell proliferation inhibition assay (MTT), Lactate dehydrogenase (LDH) assay and Hoechst staining (apoptosis). An improved apoptotic cell number was observed in Hoechst staining using compounds 9 e and 9 h further corroborated by LDH assay. Current work supports to conclude the promising ability of the title compounds to induce apoptosis through nuclear fragmentation of breast cancer cells by regulating their metabolic functions.[a] Dr.
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