نتایج جستجو برای: inhibitory concentration 50
تعداد نتایج: 882418 فیلتر نتایج به سال:
Cytotoxicity assays of immortalized lymphoblastoid cell lines (LCLs) represent a promising new in vitro approach in pharmacogenomics research. However, previous studies employing LCLs in gene mapping have used simple association methods, which may not adequately capture the true differences in non-linear response profiles between genotypes. Two common approaches summarize each dose-response cur...
New anthracycline antibiotics 3'-O-demethyl mutactimycin (3) and 4-O,3'-O-didemethyl mutactimycin (4) were isolated from two actinomycetes strains, Nocardia transvalensis and Streptomyces sp. GW 60/1571. The chemical structures were elucidated by mass spectrometry and NMR spectroscopy. Antibiotic 3 displayed moderate antimicrobial activity against Gram-positive bacteria and cytotoxicity against...
Eight platinum(II) complexes with anticancer potential have been synthesised and characterised. These complexes are of the type [Pt(I(L))(A(L))](2+), where I(L) is either dipyrido[3,2-f:2',3'-h]quinoxaline (dpq) or 2,3-dimethyl-dpq (23Me2dpq) and A(L) is one of the R,R or S,S isomers of either 1,2-diaminocyclohexane (SS-dach or RR-dach) or 1,2-diaminocyclopentane (SS-dacp or RR-dacp). The CT-DN...
Phytochemical investigation of the twigs of Chaenomeles sinensis led to the isolation and identification of six new lignan glycosides, chaenomiside A-F (1-6), along with five known ones (7-11). Their chemical structures were determined by spectroscopic methods, including NMR, MS, ECD, and GC/MS analyses. All the isolated compounds (1-11) were tested for their inhibitory effects on nitric oxide ...
In our course of screening for novel proteasome inhibitors, TMC-95A and its diastereomers, TMC-95Bto D, were isolated from the fermentation broth of Apiospora montagnei Sacc. TC 1093. TMC-95Ainhibited the chymotrypsin-like (ChT-L), trypsin-like (TL), and peptidylglutamyl-peptide hydrolyzing (PGPH) activities of 20S proteasome with IC50 values of 5.4nM, 200nM, and 60nM, respectively. TMC-95Binhi...
A series of novel 2,4-diaminoquinazoline derivatives were designed, synthesized, and evaluated as p21-activated kinase 4 (PAK4) inhibitors. All compounds showed significant inhibitory activity against PAK4 (half-maximal inhibitory concentration IC50 < 1 μM). Among them, compounds 8d and 9c demonstrated the most potent inhibitory activity against PAK4 (IC50 = 0.060 μM and 0.068 μM, respectively)...
Two new cembranes, columnariols A (1) and B (2), were isolated from the cultured soft coral Nephthea columnaris. The structures of cembranes 1 and 2 were elucidated by spectroscopic methods. In the anti-inflammatory effects test, cembranes 1 and 2 were found to significantly inhibit the accumulation of the pro-inflammatory iNOS and COX-2 protein of the lipopolysaccharide (LPS)-stimulated RAW264...
Tubulysins, linear tetrapeptides produced by several strains of myxobacteria, show an extremely high toxicity towards a wide range of cancer cell lines, with IC50 values in the nano or even picomolar range. Therefore, tubulysins and their derivatives might be suitable candidates for the development of antitumor drugs. Several synthetic approaches for tubulysins and derivates have been developed...
Ustiloxin D, produced by the rice plant pathogen Ustilaginoidea virens, exhibits potent anti-tubulin activity. In order to elucidate the effects of functional groups in ustiloxin D on its activity, several derivatives were synthesized and their anti-tubulin activities were estimated. The N,N-dimethylamino derivative and the 14-O-methyl derivative were inactive (IC50 > 50 microM). 20-Hydroxymeth...
Five new phenolic compounds rynchopeterines A-E (1-5), in addition to thirteen known phenolics, were isolated from Blaps rynchopetera Fairmaire, a kind of medicinal insect utilized by the Yi Nationality in Yunnan Province of China. Their structures were established on the basis of extensive spectroscopic analyses (1D and 2D NMR, HR-MS, IR) along with calculated electronic circular dichroism met...
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