A5079138321- Metal complexes synthesis and properties
- Fluorine in Organic Chemistry
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- RNA Research and Splicing
- Commutative Algebra and Its Applications
- Algebraic structures and combinatorial models
- DNA and Nucleic Acid Chemistry
- Ferrocene Chemistry and Applications
- Polynomial and algebraic computation
- Synthetic Organic Chemistry Methods
- Mitochondrial Function and Pathology
- Algebraic Geometry and Number Theory
- Tuberculosis Research and Epidemiology
- RNA modifications and cancer
- Cardiac Fibrosis and Remodeling
- Inorganic and Organometallic Chemistry
- Cyclopropane Reaction Mechanisms
- RNA and protein synthesis mechanisms
- Signaling Pathways in Disease
- Click Chemistry and Applications
- Synthesis and biological activity
- Granular flow and fluidized beds
- Bacteriophages and microbial interactions
- Catalytic C–H Functionalization Methods
University of North Carolina at Chapel Hill
2015-2025
Indian Institute of Technology Madras
2025
University of Tennessee Health Science Center
2025
University of Mississippi
2018-2024
Bharati Vidyapeeth Deemed University
2022
University of California, San Francisco
2011-2021
Bridge University
2020
National Institute of Technology Rourkela
2019
University of Kansas
2013-2018
Presidency University
2018
Chemical nucleases based on the transition-metal ions cleave DNA hydrolytically and/or oxidatively, with or without added reductant. We report here novel cleavage properties of highly water-soluble, square-planar [Cu(Hpyrimol)Cl] complex, together results cytotoxicities toward selected cancer cell lines. The copper complex cleaves PhiX174 supercoiled efficiently any reductant and shows high L1210 murine leukemia A2780 human ovarian carcinoma lines that are sensitive resistant to cisplatin....
Abstract Patients diagnosed with metastatic breast cancer have a dismal 5-year survival rate of only 24%. The RNA-binding protein Hu antigen R (HuR) is upregulated in cancer, and elevated cytoplasmic HuR correlates high-grade tumors poor clinical outcome cancer. promotes tumorigenesis by regulating numerous proto-oncogenes, growth factors, cytokines that support major tumor hallmarks including invasion metastasis. Here, we report inhibitor KH-3, which potently suppresses cell invasion....
Nature possesses an inexhaustible reservoir of agents that could serve as alternatives to combat the growing threat antimicrobial resistance (AMR). While some most effective drugs for treating bacterial infections originate from natural sources, they have predominantly been derived fungal and species. However, a substantial body literature is available on promising antibacterial properties plant-derived compounds. In this comprehensive review, we address major challenges associated with...
Abstract Phenanthroline derivatives are of interest due to their potential activity against cancer, and viral, bacterial, fungal infections. In a search for highly specific antitumor antibacterial compounds, we report the activities 1,10‐phenanthroline‐5,6‐dione (phendione or L 1 ), dipyrido[3,2‐ :2′,3′‐ c ]phenazine (dppz 2 corresponding platinum complexes ([PtL Cl ] [PtL ]), provide solid‐state 3D structure ]. It is generally known that toxic metal ion coordinated an active organic moiety...
The reactions of the ligand 2-(2-pyridyl)benzthiazole (pbt) with CuBr2 and ZnCl2 in acetonitrile produce complexes [Cu(pbt)Br2] (1) [Zn(pbt)Cl2] (3), respectively. When complex 1 is dissolved DMF, 2 obtained as light-green crystals. reaction pbt DMF also yields [Cu(pbt)Br2(dmf)] (2) (dmf = dimethylformamide). Complexes 1−3 were characterized by X-ray crystallography. 3 have distorted tetrahedral coordination environments, constituted two slightly different copper centers, both exhibiting...
Abstract Human antigen (Hu) R is an RNA-binding protein whose overexpression in human cancer correlates with aggressive disease, drug resistance, and poor prognosis. HuR inhibition has profound anticancer activity. Pharmacologic inhibitors can overcome the limitations of genetic inhibition. In this study, we examined antitumor activity CMLD-2, a small-molecule inhibitor directed against HuR, using non-small cell lung (NSCLC) as model. CMLD-2 efficacy was tested vitro H1299, A549, HCC827,...
Coronaviruses are viral infections that have a significant ability to impact human health. produced two pandemics and one epidemic in the last decades. The current pandemic has created worldwide catastrophe threatening lives of over 15 million as July 2020. Current research efforts been focused on producing vaccine or repurposing drug compounds develop therapeutic. There is, however, need study active site preferences relevant targets, such SARS-CoV-2 main protease (SARS-CoV-2 Mpro),...
RNA binding proteins represent an emerging class of with a role in cardiac dysfunction. We show that activation the protein human antigen R (HuR) is increased failing heart. To determine functional HuR pathological hypertrophy, we created inducible cardiomyocyte-specific HuR-deletion mouse and showed deletion reduces left ventricular dilation, fibrosis while preserving function transverse aortic constriction (TAC) model pressure overload–induced hypertrophy. Assessment HuR-dependent changes...
Abstract Hu antigen R (HuR) is indeed one of the most studied RNA-binding protein (RBP) since its fundamental role both in tumorigenesis and cancer progression. For this reason, downregulation HuR levels or inhibition biological function are, nowadays, attractive goals research. Here, we examined antitumor effects CMLD-2 four thyroid cell lines (SW1736, 8505 C, BCPAP K1). Indeed, competitively binds disrupting interaction with RNA-targets. 35 μM CLMD-2 produced a significant viability,...
The RNA-binding protein Hu antigen R (HuR) is a post-transcriptional regulator critical in several types of diseases, including cancer, making it promising therapeutic target. We have identified small-molecule inhibitors HuR through screening approach used combination with fragment analysis. A total 36 new compounds originating from linking or structural optimization were studied to establish structure–activity relationships the set. Two top inhibitors, 1c and 7c, further validated by...
A convergent synthesis of the C(18)−C(34) fragment amphidinolide C and C(18)−C(29) F is reported. The approach involves common intermediate tetrahydrofuranyl-β-ketophosphonate via cross metathesis, Pd(0)-catalyzed cyclization, hydroboration−oxidation. β-ketophosphonate was coupled to three side chain aldehydes using a Horner−Wadsworth−Emmons (HWE) olefination reaction give dienones, which were reduced with l-selectride fragments F.
Venezuelan equine encephalitis virus (VEEV) is an emerging pathogenic alphavirus that can cause significant disease in humans. Given the absence of therapeutic options available and significance VEEV as a weaponized agent, optimization effort was initiated around quinazolinone screening hit 1 with promising cellular antiviral activity (EC50 = 0.8 μM), limited cytotoxic liability (CC50 > 50 modest vitro efficacy reducing viral progeny (63-fold at 5 μM). Scaffold revealed novel rearrangement...
Abstract The mitochondrial permeability transition pore (mtPTP) is a Ca 2+ ‐requiring mega‐channel which, under pathological conditions, leads to the deregulated release of and dysfunction, ultimately resulting in cell death. Although mtPTP potential therapeutic target for many human pathologies, its as drug currently unrealized. Herein we describe an optimization effort initiated around hit 1 , 5‐(3‐hydroxyphenyl)‐ N ‐(3,4,5‐trimethoxyphenyl)isoxazole‐3‐carboxamide, which was found possess...
ABSTRACT MraY, a bacterial enzyme crucial for the synthesis of peptidoglycans, represents promising yet underexplored target development effective antibacterial agents. Nature has provided several classes nucleoside inhibitors MraY and scientists have modified these structures further to obtain natural product-like MraY. The products their synthetic analogs suffer from non-optimal in vivo efficacy, complexity renders structure-activity relationship (SAR) studies molecules particularly...
Abstract The RNA‐binding protein human antigen R (HuR) has been shown to reduce cardiac remodeling following both myocardial infarction and pressure overload, but the full extent of HuR‐dependent mechanisms within cells myocardium yet be elucidated. Wild‐type mice were subjected 30 min ischemia (via LAD occlusion) treated with a novel small molecule inhibitor HuR at time reperfusion, followed by direct in vivo assessment structure function. Direct was done vitro using neonatal rat...
Abstract A density function for an algebraic invariant is a measurable on which measures the ‐scale. This carries lot more information related to without seeking extra data. It has turned out be useful tool, was introduced by third author in Trivedi [Trans. Amer. Math. Soc. 370 (2018), no. 12, 8403–8428], study characteristic invariant, namely Hilbert–Kunz multiplicity of homogeneous ‐primary ideal. Here, we construct functions Noetherian filtration ideals and given saturated powers ideal...
The reaction of the redox-active ligand, Hpyramol (4-methyl-2-N-(2-pyridylmethyl)aminophenol) with K2PtCl4 yields monofunctional square-planar [Pt(pyrimol)Cl], PtL-Cl, which was structurally characterised by single-crystal X-ray diffraction and NMR spectroscopy. This compound unexpectedly cleaves supercoiled double-stranded DNA stoichiometrically oxidatively, in a non-specific manner without any external reductant added, under physiological conditions. Spectro-electrochemical investigations...
Abstract Persistent opening of the mitochondrial permeability transition pore (PTP), an inner membrane channel, leads to dysfunction and renders PTP a therapeutic target for host life‐threatening diseases. Herein, we report our effort toward identifying small‐molecule inhibitors this through structure–activity relationship optimization studies, which led identification several potent analogues around N ‐phenylbenzamide compound series identified by high‐throughput screening. In particular, 4...
This TFA-catalyzed [3+2] cycloaddition of organic azides with α-fluoronitroalkenes, used as synthetic surrogates α-fluoroalkynes, provides a new route to multi-substituted fluorotriazoles broader substrate scopes and high regioselectivity.
Tumor suppressor ARID1A, a subunit of the chromatin remodeling complex SWI/SNF, regulates cell cycle progression, interacts with tumor TP53, and prevents genomic instability. In addition, ARID1A has been shown to foster resistance cancer therapy. By promoting non-homologous end joining (NHEJ), enhances DNA repair. Consequently, proposed as promising therapeutic target sensitize cells chemotherapy radiation. Here, we report that is regulated by human antigen R (HuR), an RNA-binding protein...
Short, high yielding syntheses of both diastereomers the naturally occurring oxylipids 1 and 2 using a combination organocatalytic hydroxylation an aldehyde, alkene cross metathesis, palladium(0) catalyzed cyclization chemistry (six-step process) are reported. Furthermore, influence catalyst on metathesis reaction homoallylic 1,2-diol has been studied in detail.
Molecular assessments at the single cell level can accelerate biological research by providing detailed of cellular organization and tissue heterogeneity in both disease health. The human kidney has complex multi-cellular states with varying functionality, much which now be completely harnessed recent technological advances proteomics a near single-cell level. We discuss foundational steps first application this mass spectrometry (MS) based method for analysis sub-sections normal kidney, as...
SUMMARY Infection of a susceptible host with Leishmania, protozoan parasite, causes the disease leishmaniasis, which is characterized by neutrophil, eosinophil, macrophage, lymphocyte and mast cell infiltration into infected tissue followed parasite growth. Although roles played other cells in leishmaniasis are known, role remains to be ascertained. Here, we demonstrate that Leishmania regulates site infection, production function resulting differential growth resistant (C57BL/6 or CBA/T6T6)...