Nanotherapeutics made revolutionary changes in healthcare as well as provide a vision to empower diagnostics and treatment strategies because of its ability to control the release of enclosed bioactive compound. It has gained special attention in modern medical research because of its potential ...
6-Methyl-1-({[(2E)-2-methyl-3-phenyl-prop-2-en-1-yl]oxy}methyl)-1,2,3,4-tetra-hydro quinazoline-2,4-dione was prepared via treatment of silylated 6-methylquinazoline-2,4-dione with bis-[(E)-2-methyl-3-phenylallyloxy]methane. FT-IR and FT-Raman spectra were recorded and analyzed. The vibrational ...
We describe an extensive SAR study in the 6-[4-fluoro-3-(substituted)benzyl]-4,5-dimethylpyridazin-3(2H)-one series which led to the identification of potent PARP-1 inhibitors, capable of inhibiting the proliferation of BRCA-1 deficient cancer cells in the low nanomolar range, and displaying >10...
A series of benzofuran-2-carboxamide-N-benzyl pyridinium halide derivatives (6a-o) are synthesized as new cholinesterase inhibitors. The synthetic pathway involves the reaction of salicylaldehyde derivatives and ethyl bromoacetate, followed by hydrolysis and amidation with 3- and 4-picolyl amine...
Leukemia is the most common blood cancer, and its development starts at diverse points, leading to distinct subtypes that respond differently to therapy. This heterogeneity is rarely taken into account in therapies, so it is still essential to look for new specific drugs for leukemia subtypes or...
Despite the success achieved in the treatment of acute lymphoblastic leukemia (ALL), the search for new drugs featuring selectivity against leukemia cells and effectiveness to prevent relapsed ALL is still highly desirable. Here, we described the synthesis of several novel 3-substituted and 3,6-...
A novel series of methyl indolinone-6-carboxylates bearing an indole moiety were identified as potent angiokinase inhibitors. The most active compound, A8, potently targeted the kinase activities of vascular endothelial growth factor receptors 2 and 3, and platelet-derived growth factor receptor...
An efficient protocol for highly chemoselective introduction of dithiocarbamate groups to nitrogen position of indoles with bis(dialkylaminethiocarbonyl)disulfides was achieved by employing t-BuOK as a promoter. Based on this methodology, twenty nine novel indole-dithiocarbamate compounds were p...
Compounds having a partial 2-pyridone structure or 3-pyridazinones can be selectively N-arylated with phenylboronic acids according to the procedure described by Chan and Lam. This procedure leads to N5-arylated imidazo[4,5-c]pyridin-4-ones, precursors of potent factor Xa inhibitors. In addition...
This report describes the synthesis, and in vitro and in vivo antimalarial evaluations of certain ester-modified neocryptolepine (5-methyl-5H-indolo[2,3-b]quinoline) derivatives. The modifications were carried out by introducing ester groups at the C2 and/or C9 position on the neocryptolepine co...
Solid lipid nanoparticles (SLNs) with complex internal phase were fabricated for formulating stavudine (D4T), delavirdine (DLV), and saquinavir (SQV). The lipids including Compritol 888 ATO, tripalmitin, and cacao butter were stabilized by l-α-phospatidylcholine, cholesteryl hemisuccinate, and ...
Background: Cross resistance is common among the non-nucleoside reverse transcriptase inhibitors (NNRTIs). G190A appears in 5–15% of the patients treated with nevirapine or efavirenz who develop clinical resistance. Objectives: In this study we investigated the effect of G190A and other NNRTI s...
The objective of the study was to investigate the safety and antiviral effect of three delavirdine dose regimens or placebo in combination with zidovudine in patients who were already taking zidovudine. Eighty-nine symptomatic HIV-1 seropositive individuals with CD4+ cell counts between 50 and 3...
This study was performed to determine delavirdine protein-binding characteristics as well as those of its N-dealkylated metabolite (N-DLV). Initial studies of 36 μM delavirdine and 30 μM N-DLV in solutions of plasma, albumin 4 g%, alpha-1-acid glycoprotein (AAG) 100 mg% or immune globulin (IVI...
The design and synthesis of a novel conformationally constrained spiro analog of the BHAP class of HIV-1 reverse transcriptase inhibitors, based on the molecular modeling and the X-ray crystal structure of the clinical candidate atevirdine, is described.
Rationale: To determine the dosage requirements and pharmacokinetics of atevirdine, a non-nucleoside reverse transcriptase inhibitor and its N-dealkylated metabolite (N-ATV) during phase I studies in patients receiving atevirdine alone or in combination with zidovudine. Design: Two open label, p...
A sensitive reversed-phase high-performance liquid chromatographic method for the determination of atevirdine and its primary metabolite in human saliva or cerebrospinal fluid using solid-phase extraction is described. Samples mixed with internal standard and sodium phosphate buffer were applied...
The in vitro protein-binding characteristics of atevirdine (ATV), a non-nucleoside reverse transcriptase inhibitor with activity against HIV-1, and its N-dealkylated metabolite (N-ATV) were studied using equilibrium dialysis. ATV and N-ATV were studied at concentrations of 5, 10, 20, and 30 μM ...
A group of N-acetyl-2-(or 3-)carboxymethylbenzenesulfonamides, possessing either a F or a substituted-phenyl ring substituent (4-F, 2,4-F2, 4-SO2Me, 4-OCHMe2) attached to its C-4 or C-6 position, was prepared using a palladium-catalyzed Suzuki cross-coupling reaction for evaluation as selective ...
N-Acetyl-2-carboxybenzenesulfonamide (11), and a group of analogues possessing an appropriately substituted-phenyl substituent (4-F, 2,4-F2, 4-SO2Me, 4-OCHMe2) attached to its C-4, or C-5 position, were synthesized for evaluation as selective cyclooxygenase-2 (COX-2) inhibitors. In vitro COX-1/C...
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