133 research outputs found
Glycoside cluster effects on antibody recognition of MUC1 glycopeptides [an abstract of dissertation and a summary of dissertation review]
No full text
Novel 1,3,4-oxadiazole induces anticancer activity by targeting NF-KB in hepatocellular carcinoma cells
No full textAberrant activation of NF-κB is linked with the progression of human malignancies including hepatocellular carcinoma (HCC), and blockade of NF-κB signaling could be a potential target in the treatment of several cancers. Therefore, designing of novel small molecule inhibitors that target NF-κB activation is of prime importance in the treatment of several cancers. In the present work, we report the synthesis of series of 1,3,4-oxadiazoles, investigated their anticancer potential against HCC cells, and identified 2-(3-chlorobenzo[b]thiophen-2-yl)-5-(3-methoxyphenyl)-1,3,4-oxadiazole (CMO) as the lead compound. Further, we examined the effect of CMO on cell cycle distribution (flow cytometry), apoptosis (annexin V-propidium iodide-FITC staining), and phosphorylation of NF-κB signaling pathway proteins (IκB and p65) in HCC cells. We found that CMO induced antiproliferative effect in dose- and time-dependent manner. Also, CMO significantly increased the percentage of sub-G1 cell population and induced apoptosis. Furthermore, CMO found to decrease the phosphorylation of IκB (Ser 32) in the cytoplasmic extract and p65 (Ser 536) in the nuclear extract of HCC cells. It also abrogated the DNA binding ability and transcriptional activity of NF-κB. CMO induced the cleavage of PARP and caspase-3 in a time-dependent manner. In addition, transfection with p65 small interfering RNA blocks CMO-induced caspase-3/7 activation. Molecular docking analysis revealed that CMO interacts with the hydrophobic region of p65 protein. Thus, we are reporting CMO as an inhibitor of NF-κB signaling pathway. © 2018 Mohan, Anilkumar, Rangappa, Shanmugam, Mishra, Chinnathambi, Alharbi, Bhattacharjee, Sethi, Kumar, Basappa and Rangappa
Identification of beta-aminopyrrolidine containing peptides as beta-amyloid aggregation inhibitors for Alzheimer's disease
No full textAlzheimer's disease (AD) is caused by a series of events initiated by the production and aggregation of the amyloid beta-protein (A beta). In the early stages of the disease, A beta is released in a soluble form then progressively forms oligomeric, multimeric, and fibrillar aggregates, triggering neurodegeneration. Thus, development of inhibitors that initiate reverse A beta aggregation is thought to be a logical approach in treating AD. In this context, we developed beta-aminopyrrolidine containing 12 mer peptide 3 which is very potent in inhibiting the A beta aggregation and also reducing A beta(42)-induced cytotoxicity
A green synthesis of 1,5-benzodiazepines using reusable-heterogeneous silica sulfuric acid catalyst under solvent-free conditions and their antileukemic activity
No full textA trisubstituted pyrazole derivative reduces DMBA-induced mammary tumor growth in rats by inhibiting estrogen receptor-α expression
No full textAberrant expression of estrogen receptor alpha (ER-α) is observed in many pathological complications like breast cancer, endometrial cancer, and in osteoporosis. ER-α plays a vital role in the initiation and progression of breast cancer and confers chemo and radioresistance to the cancer cells by upregulating expression of anti-apoptotic proteins. The synthetic pyrazole derivative 3-(1-(4-bromophenyl)-5-phenyl-1H-pyrazol-3-yl)pyridine (compound 5d) displays significant cytotoxicity against mammary carcinoma cells. Molecular docking studies revealed that compound 5d binds to ligand binding domain of (ER-α). In vivo studies were carried out to investigate ER-α expression by immunohistochemistry and quantitative RT-PCR, which revealed reduction of ER-α in tumor cells upon treatment with compound 5d indicating its ER-α antagonistic effect. Our study ascertains compound 5d as a potent inhibitor of mammary carcinoma cells
Efficient One‐Pot Synthesis of 3,5‐Disubstituted 1,3,4‐Thiadiazole from Dithioesters under Mild Condition
No full textAn easy and efficient method for the synthesis of quinoxalines using recyclable and heterogeneous nanomagnetic‐supported acid catalyst under solvent‐free condition
No full textSynthesis of quinoxalines from o‐phenylenediamines (o‐PDs) with electronically diversified 1,2‐diketones and α‐bromoketones via simple cyclocondensation reaction using an heterogeneous nano‐ϒ‐Fe2O3‐SO3H catalyst has been reported under solvent free condition. Low cost, easy workup, high yield, operational simplicity, less reaction time, environmentally benign nature and catalyst is magnetically retrievable and can be reused up to five catalytic cycles without significant loss in the product yields are the noteworthy features of this protocol
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