A5079654159- Synthesis and biological activity
- Crystallization and Solubility Studies
- Tuberculosis Research and Epidemiology
- Chemical Synthesis and Analysis
- Click Chemistry and Applications
- Computational Drug Discovery Methods
- Multicomponent Synthesis of Heterocycles
- Chemical Synthesis and Reactions
- Synthesis and Characterization of Heterocyclic Compounds
- Asymmetric Synthesis and Catalysis
- Cancer therapeutics and mechanisms
- Drug Solubulity and Delivery Systems
- Antimicrobial Peptides and Activities
- X-ray Diffraction in Crystallography
- Synthesis and Biological Evaluation
- Carbohydrate Chemistry and Synthesis
- Phosphodiesterase function and regulation
- Oxidative Organic Chemistry Reactions
- Phenothiazines and Benzothiazines Synthesis and Activities
- Sulfur-Based Synthesis Techniques
- Antimicrobial agents and applications
- Quinazolinone synthesis and applications
- Catalytic C–H Functionalization Methods
- Histone Deacetylase Inhibitors Research
- Antimicrobial Resistance in Staphylococcus
Manipal Academy of Higher Education
2016-2025
Lupin Pharmaceuticals (India)
2016
Netaji Subhas University of Technology
2014
National Institute of Allergy and Infectious Diseases
2005
St. Jude Children's Research Hospital
2005
GlaxoSmithKline (United Kingdom)
2005
National Institutes of Health
2004-2005
University of Mumbai
1989
Non-small cell lung carcinomas (NSCLC) are the predominant form of malignancy and reason for highest number cancer-related deaths. Widespread deregulation Akt, a serine/threonine kinase, has been reported in NSCLC. Allosteric Akt inhibitors bind space separating Pleckstrin homology (PH) catalytic domains, typically with tryptophan residue (Trp-80). This could decrease regulatory site phosphorylation by stabilizing PH-in conformation. Hence, this study, computational investigation was...
<title>Abstract</title> KDM5B, a lysine-specific histone demethylase, is widely upregulated in breast cancer. The current study investigated the role of KDM5B cancer and explored repurposing potential antiviral drug abacavir (ABC). cytotoxic effects effect ABC sensitization on doxorubicin (DOX) efficacy were evaluated using 2-D 3-D cell culture models. expression was elevated tissues compared to normal tissues. <italic>In vitro</italic> studies demonstrated that treatment reduced cells...
We have described the synthesis of new 1,2,4-triazoles and evaluated their antimicrobial profile. Antitubercular activity was determined in triplicate using Lowenstein-Jensen medium. A loopful Mycobacterium tuberculosis suspension inoculated on surface each media containing test compounds (100, 10 or 1 microg mL(-1)). To evaluate in-vitro antibacterial activity, (50, 5 0.5 microg) were against B. subtilis, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus typhi by disc...
Thiolactomycin inhibits bacterial cell growth through inhibition of the β-ketoacyl-ACP synthase activity type II fatty acid synthases. The effect modifications 5-position isoprenoid side chain on both IC50 and MIC were determined. Synthesis screening a structurally diverse set analogues revealed very little tolerance for substitution in purified enzyme assays, but few retained MIC, presumably another target. Even subtle such as reducing one or double bonds diene not tolerated. only...
The aligned manuscript reports synthesis, screening and QSAR analysis of twenty six 1, 2, 4-triazole analogues from their respective aromatic carboxylic acids. structures synthesized were characterized using physical spectral analysis. 4-Triazole analogs antioxidant capacity was determined DPPH radical scavenging assay. Results revealed that out L, T & VRT series, series 4-triazoles have significant activities when compared with standard ascorbic acid. To obtain structural insights for...
Novel Triclosan mimic diphenyl ether derivatives 4a–k were designed and synthesized with lipophilicity considerably lesser than that of Triclosan. The binding mode the compounds at active site enoyl-ACP reductase was analysed using docking method. syntheses carried out one-pot reductive amination reaction characterized by spectral techniques. evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv strain Microplate Alamar Blue assay. Compounds 4h 4j most...
Dietary polyphenols such as quercetin and curcumin have been extensively administered to patients with cancer in the form of herbal supplements. They may a synergistic anticancer effect; however, risk pharmacokinetic interactions selective CDK-4/6 inhibitors that are metabolized by CYP3A4 enzyme exists. Considering these aspects, current study examined effects on human ascertain CYP3A4-mediated herb-drug CDK inhibitors. In this study, using silico methods inhibition kinetics liver microsomes...
Iron-based metal-organic frameworks (MIL (101)) have recently gained attention in materials science for biomedical applications. In the present work, MOF (MIL-101(Fe)) were coated with lactoferrin (Lf) conjugated hyaluronic acid (HA) and investigated its potential delivering 5-fluorouracil (5-FU), along assessing toxicity profile. The synthesised nanoparticles extensively characterised using spectroscopic, X-Ray, thermal electron microscopic techniques. 5-FU was loaded into MOFs,...
Lichens are symbiotic organisms that have been traditionally used for treating different kinds of ailments. As there only a few reports on the antiviral activity lichens, we thought evaluating anti-Herpes simplex virus-1 (HSV-1) methanolic extract Roccella montagnei and their isolated compounds. Fractionation crude by column chromatography two pure Antiviral was assessed using CPE inhibition assay at non-cytotoxic concentrations Vero cells. Molecular docking dynamics studies were carried out...
Palbociclib and ribociclib are substrates of efflux transporter P-glycoprotein which plays a key role in absorption transport these drugs. Proton pump inhibitors, when co-administered with them known to show inhibitory effect on P-glycoprotein.Therefore, this study aims investigate the proton inhibitors inhibition mediated palbociclib ribociclib.A combined approach molecular docking ex vivo everted gut sac model was implemented predict potential i.e., omeprazole, esomeprazole, lansoprazole,...
In our efforts to develop druggable diphenyl ethers as potential antitubercular agents, a series of novel ether derivatives ( 5a – f , 6a ) were designed and synthesized. The representative compounds showed promising in vitro activity against drug‐susceptible, isoniazid‐resistant, multidrug‐resistant strains Mycobacterium tuberculosis with MIC values 1.56 μg/ml 6b ), 6.25 6a–d 3.125 6b–c respectively. All the synthesized exhibited satisfactory safety profile CC 50 > 300 μg/ml) Vero HepG2...
This computational study exclusively illustrates the key molecular features of bedaquiline and its analogues required for binding to mycobacterial ATP synthase.
We describe a facile, sustainable, and chemoselective process for the synthesis of unsymmetrical (thio)ureas through "on-water" reaction (thio)isocyanates with amines. Detailed mechanistic studies revealed that physical nature solubility reagents in water are responsible observed rate selectivity. Significant efforts have been made to design scalable achieve "zero waste" "water-mediated" protocol from The decisive advantages simple product isolation filtration recycling effluent. It also...