Search Results - "Adla, Santosh Kumar"
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Current approaches to facilitate improved drug delivery to the central nervous system
Published in European journal of pharmaceutics and biopharmaceutics (01-12-2022)“…[Display omitted] Although many pharmaceuticals have therapeutic potentials for central nervous system (CNS) diseases, few of these agents have been…”
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Comparative Modelling of Organic Anion Transporting Polypeptides: Structural Insights and Comparison of Binding Modes
Published in Molecules (Basel, Switzerland) (03-12-2022)“…To better understand the functionality of organic anion transporting polypeptides (OATPs) and to design new ligands, reliable structural data of each OATP is…”
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Ganciclovir and Its Hemocompatible More Lipophilic Derivative Can Enhance the Apoptotic Effects of Methotrexate by Inhibiting Breast Cancer Resistance Protein (BCRP)
Published in International journal of molecular sciences (20-07-2021)“…Efflux transporters, namely ATP-binding cassette (ABC), are one of the primary reasons for cancer chemoresistance and the clinical failure of chemotherapy…”
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Neurosteroids: Structure-Uptake Relationships and Computational Modeling of Organic Anion Transporting Polypeptides (OATP)1A2
Published in Molecules (Basel, Switzerland) (17-09-2021)“…In this study, we investigated the delivery of synthetic neurosteroids into MCF-7 human breast adenocarcinoma cells via Organic Anionic Transporting…”
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Increased/Targeted Brain (Pro)Drug Delivery via Utilization of Solute Carriers (SLCs)
Published in Pharmaceutics (10-06-2022)“…Membrane transporters have a crucial role in compounds’ brain drug delivery. They allow not only the penetration of a wide variety of different compounds to…”
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Strong Inhibitory Effect, Low Cytotoxicity and High Plasma Stability of Steroidal Inhibitors of N -Methyl-D-Aspartate Receptors With C-3 Amide Structural Motif
Published in Frontiers in pharmacology (12-11-2018)“…Herein, we report the synthesis, structure-activity relationship study, and biological evaluation of neurosteroid inhibitors of -methyl-D-aspartate receptors…”
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Novel inhibitors of bromodomain and extra-terminal domain trigger cell death in breast cancer cell lines
Published in Bioorganic & medicinal chemistry (01-10-2024)“…[Display omitted] •Novel scaffolds for the development of the bromodomain and extra-terminal domain (BET) inhibitors.•Some compounds also inhibited Sirtuins…”
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Amino acid transporters in neurological disorders and neuroprotective effects of cysteine derivatives
Published in Neurochemistry international (01-07-2024)“…For most diseases and disorders occurring in the brain, the full causes behind them are yet unknown, but many show signs of dysfunction of amino acid…”
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Current Chemical, Biological, and Physiological Views in the Development of Successful Brain-Targeted Pharmaceutics
Published in Neurotherapeutics (01-04-2022)“…One of the greatest challenges with successful pharmaceutical treatments of central nervous system (CNS) diseases is the delivery of drugs into their target…”
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5β-reduced neuroactive steroids as modulators of growth and viability of postnatal neurons and glia
Published in The Journal of steroid biochemistry and molecular biology (01-05-2024)“…Endogenous neurosteroids (NS) and their synthetic analogs, neuroactive steroids (NAS), are potentially useful drug-like compounds affecting the pathophysiology…”
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Targeting Glial Cells by Organic Anion-Transporting Polypeptide 1C1 (OATP1C1)-Utilizing l-Thyroxine-Derived Prodrugs
Published in Journal of medicinal chemistry (23-11-2023)“…OATP1C1 (organic anion-transporting polypeptide 1C1) transports thyroid hormones, particularly thyroxine (T ), into human astrocytes. In this study, we…”
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Indole prenylation in alkaloid synthesis
Published in Topics in current chemistry (01-01-2012)“…Important biologically active indole alkaloids are decorated with prenyl (3,3-dimethylallyl) and tert-prenyl (1,1-dimethylallyl) groups. Covering the…”
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Altering distribution profile of palbociclib by its prodrugs
Published in European journal of pharmaceutical sciences (01-01-2024)“…Palbociclib, a cyclin-dependent kinase (CDK) 4/6 inhibitor, is currently used clinically for treating hormone receptor-positive and human epidermal growth…”
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Screening of novel 3α5β-neurosteroids for neuroprotective activity against glutamate- or NMDA-induced excitotoxicity
Published in The Journal of steroid biochemistry and molecular biology (01-05-2019)“…[Display omitted] •3α5β-Neurosteroids suppress both glutamate- and NMDA-induced excitotoxicity.•Ca2+ entry and consequent ROS release and caspase-3 activation…”
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Synthesis of carbocyclic analogs of dehydroaltenusin: identification of a stable inhibitor of calf DNA polymerase α
Published in Tetrahedron (07-10-2015)“…Syntheses of carbocyclic analogs of dehydroaltenusin tautomers are reported. Both target compounds, cDHA…”
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Doubly prenylated tryptamines: cytotoxicity, antimicrobial activity and cyclisation to the marine natural product flustramine A
Published in Organic & biomolecular chemistry (28-09-2013)“…The marine natural product flustramine A was synthesised via oxidative cyclisation of Nb-methylated 1-prenyl-2-tert-prenyl-6-bromotryptamine and subsequent…”
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Physicochemical and biological properties of novel amide-based steroidal inhibitors of NMDA receptors
Published in Steroids (01-01-2017)“…[Display omitted] •Synthesis of new amide-based inhibitors of NMDA receptors.•Strong inhibitors of NMDA currents.•The Caco-2 assay was used to evaluate…”
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Diastereoselective Flexible Synthesis of Carbocyclic C‑Nucleosides
Published in Journal of organic chemistry (07-04-2017)“…Carbocyclic C-nucleosides are quite rare. Our route enables flexible preparation of three classes of these nucleoside analogs from common precursors–properly…”
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