Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 20 of 497 for “"IC50"”.
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Design, synthesis, and structure-activity relationship studies of dual Plasmodium falciparum phosphatidylinositol 4-kinase and cGMP-dependent protein kinase inhibitors
… inhibition. Notable analogues included 7 (PfNF54 IC50 = 0.029 µM; PvPI4K IC50 = 0.007 µM; PfPKG IC50 > 2 µM) and 35 (PfNF54 IC50 = 0.086 µM; PvPI4K IC50 = 0.008 µM; PfPKG IC50 > 10 µM). Introduction of basic or pyridyl substituents proved important for dual Plasmodium kinase activity as …
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Novel Modulators of CD39 and CD73
… POM-1 for CD39 and AB680 for CD73. The IC50s of Identified leads were determined, and their mechanisms of action were analysed by examining the effects on Vmax and Km through non-linear regression. Potential modulator binding sites were identified using blind docking with CB-Dock2. This …
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Assessing the acetylcholinesterase inhibitory potential of novel pharmacophores for potential treatment of Alzheimer’s disease
… lowest half maximal inhibitory concentration (IC50) of 0.20 µM, albeit less potent than donepezil (IC50 = 0.03 µM). The SwissADME pharmacokinetic tool predicted that compounds A8, A73, A136, C53 and C129 were BBB-permeable. Synergism (combination index [CI] < 1) was observed between: ¼IC50 …
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Inhibitors of human cathepsin L and cruzain as therapeutic agents.
… cathepsin L. While most of the compounds had IC50 values in the range of 0.4 µM or greater, four were very effective inhibitors of cathepsin L: the benzophenone thiosemicarbazones 2 (IC50= 1.5 nM), 55 (IC50= 44 nM), 38 (IC50= 60 nM), 32 (IC50= 66 nM), and 37 (IC50= 140 nM) and a sulfone analog …
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Evaluation of hops essential oil cytotoxicity and anti-cryptosporidium activity
… Methods. HEO and myrcene in vitro cytotoxicity (IC50) were determined in an HCT-8 intestinal cell model using flow cytometry and staining for non-viable cells with propidium iodide after treatment with controls and different concentrations of bioactives of interest (i.e. HEO and myrcene) for 24 …
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Synthesis of Novel CYP1 Activated Heterocyclic Anticancer Prodrugs
… yl)-5-(3,4-methylenedioxyphenyl)pyrazole) gave an IC50 value of 8μM towards the MDA 468 cell line. The MCF7 cells, TCDD induced and non-induced gave IC50 values of 10μM each. Although the pyrazoles showed plausible tumour toxicity, an investigation into six membered pyrimidine heterocycles was …
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Isolation and Structure Elucidation of Anticancer and Antimalarial Natural Products
… A2780 human ovarian cancer cell line assay with IC50 values of 3 uM and 10 uM, respectively. Compound 3.1 showed potent antiplasmodial activity with an IC50 value of 100 nM, while compounds 3.2 and 4.1 showed moderate antiplasmodial activity with IC50 values of 4 uM and 10 uM, respectively. The …
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An investigation into the antineoplastic properties of Schinziophyton Rautanenii and Colophospermum mopane
… by the organic root extract of C. mopane, with IC50 48.2 μg/ml although it also showed mild cytotoxicity against fibroblast cells, IC50 162.4 μg/ml. In vivo toxicity evaluation further revealed the strong toxicity level of the organic C. mopane root extract against the freshwater flatworm …
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Isolation and Structure Elucidation of Antiproliferative and Antiplasmodial Natural Products from Plants
… the A2780 human ovarian cancer cell line with IC50 values of 6.9 uM and 3.4 uM, respectively. They also exhibited moderate antiplasmodial activity against chloroquine-resistant Plasmodium falciparum strain Dd2 with IC50 values of 9.9 ± 1.4 uM and 2.8 ± 0.7 uM, respectively. Compounds 3.1 to 3.4 …
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Synthesis of Macrocyclic Polyamines and their Cu, Fe, Mn and Zn Complexes Targeting HIV (AIDS).
… in cell cultures uncovered five leads, SH06 (IC50 = 0.41 ± 0.06 μg/mL, CC50 = 20 μg/mL), SH15 (IC50 = 0.50 ± 0.16 μg/mL, CC50 = >100 μg/mL), SH16 (IC50 = 1.23 ± 0.50 μg/mL, CC50 = 51 μg/mL), SH34 (IC50 = 0.86 ± 0.35 μg/mL, CC50 = >100 μg/mL) …
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Antimicrobial constituents of Artemisia afra Jacq. ex Willd. against periodontal pathogens
… extract showed good antioxidant activity with an IC50 value of 22.2 μg/ml. Scopoletin had a strong transformation of the DPPH radical into its reduced form, with an IC50 value of 1.24 μg/ml which was significant to that of vitamin C (1.22 μg/ml). Acacetin and Betulinic acid exhibited a decreased …
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Neurotropní a antioxidační aktivita vybraných druhů jednoděložných alkaloidních rostlin. IV.
… rostliny Narcissus Flower Record s hodnotou IC50 = 5,6 ± 2,1 µg/ml. Nejvýznamnější aktivitu vůči HuAChE i HuBuChE zároveň projevil alkaloidní extrakt z rostliny Narcissus poeticus var. recurvus s hodnotami IC50 = 6,0 ± 0,1 µg/ml pro HuAChE a IC50 = 23,0 ± 1,0 µg/ml pro HuBuChE. Izolovaný …
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Discovery and Delivery of Bioactive Natural Products
… activity, trichospirolide A with an IC50 value of 1.5 μM, malleastrumolide A with an IC50 value of 2.7 μM, and (+)-lariciresinol with an IC50 value of 3.7 μM. In addition to the studies of drug delivery of bioactive natural product, doxorubicin, a novel thiolated doxorubicin analog …
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Cytotoxic compounds from the genus Centaurea.
… shrimp lethality and MTT assay. Arctigenin (IC50=7.0 mM), matairesinol, montamine (IC50=43.9 mM) and lappol A, schischkiniin, arctiopicrin (IC50=8.5 mM) and 8-0-(4-hydroxy-3-methylbutanoyl)-salonitenolide (IC50=26.4 mM) showed higher cytotoxicity against MTT assay. Matairesinoside (IC50=2.2 x …
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Antioxidant activity and phytochemical evaluations of selected medicinal plants
… to have potent DPPH radical scavenging activity (IC50 = 48.75 ± 7.00 μg/ml). Activity-guided fractionation resulted in the isolation of three principal antioxidant compounds; acteoside, angoroside C and angoroside A. Acteoside (yield = 1.21%, IC50 = 15.2 μM) appeared to be the most abundant and …
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Development, evaluation, and In-vitro assessment of artificial intelligence antidiabetic predictive models from α-glucosidase inhibitors
… inhibitors that has experimentally determined IC50, develop ML and DL models for predicting α-glucosidase inhibitors, utilize these models for virtual screening to identify potential α-glucosidase inhibitors, and perform in vitro assays on the identified hits to validate predictions. Method: …
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In vitro evaluation of the cytotoxic potential of Brickellia cavanillesi (Asteraceae) using HepG2 cells
… cells (HepG2) were submitted to both a dose- (IC50) and a time-dependent toxicity evaluation in the presence or absence of Fetal Bovine Serum (FBS). Herbal extracts (1-35%) were used for the IC50 study. In the time course study, cells were exposed to 1-10% extract solutions of B. cavanillesi …
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Elaboration of 4′-Phosphopantetheine Adenylyltransferase inhibitors and Benzoxaboroles as antimalarial agents
… against the drugsensitive PfNF54 strain with IC50's between 1.04 µM and 2.9 µM were identified. These compounds were resynthesized but were found not to validate with the exception of one compound 2/MM1-19 from the Ugi series, albeit at 2-fold less activity than the hit (IC50 = 5.2 µM). The …
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Evaluation of Novel Carbamate Insecticides for Neurotoxicity to Non-Target Species
… control. First, 50% inhibition concentration (IC50) data was collected from three mammalian AChEs with eight commercial carbamate insecticides by using the Ellman assay. The IC50 values varied from 57 nM to 7358 nM. The AChE sensitivity pattern and level were shown to be similar between the …
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Screening Of Natural Products For Their Effect On Kallikrein-Kinin System: Potential Implications In The Treatment Of Hereditary Angioedema
… plasma kallikrein on endothelial cells with IC50 values of 15, 20, 20, 80, 160 and 400 mg/ml, respectively. T. chebula fruit, T. bellirica fruit, T. arjuna fruit, T. arjuna bark and black tea extracts blocked FXIIa activity with IC50 values of 30, 50, 190, 190 and 27 mg/ml, respectively. …
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