An extension of our previous research work has resulted in a number of new ATP-competitive CK2 inhibitors that have been identified among 4-aminothieno[2,3-d]pyrimidine derivatives. The most active compounds obtained in the course of the research are 3-(5-p-tolyl-thieno[2,3-d]pyrimidin-4-ylamino...
Herein we disclose the synthesis and SAR of a series of 4-(phenylsulfamoyl)phenylacetamide compounds as mGlu4 positive allosteric modulators (PAMs) that were identified via a functional HTS. An iterative parallel approach to these compounds culminated in the discovery of VU0364439 (11) which rep...
A V79 Chinese hamster fibroblast cell line selected for resistance to the toxic effects of 5-fluorouracil (Kaufman, 1984b) was found to be cross-resistant to the toxic effects of the thymidine analog 5-bromodeoxyuridine (BrdUrd). When tested for sensitivity to BrdUrd mutagenesis, the fluorouraci...
BackgroundThe mechanisms underlying stress-induced inflammation that contribute to major depressive disorder are unknown. We examine the role of the adenosine triphosphate (ATP)/purinergic type 2X7 receptor (P2X7R) pathway and the NLRP3 (nucleotide-binding, leucine-rich repeat, pyrin domain cont...
Resistance to 6-thioguanine was induced by 5-bromodeoxyuridine (BUdR) in synchronous Chinese hamster cells. The yield of mutant colonies was not proportional to the amount of BUdR incorporated into DNA; thus mutants were not due to mispairing of BUdR with guanine during replication. Few mutants ...
We have studied the effects of 5-bromodeoxyuridine (BrdUrd) at two genetic loci in diploid human lymphoblasts cells. In thymidine kinase heterozygotes (tk+/−), a 2-h of BrdUrd induced a transient, non-heritable resistance to the thymidine analogue, trifluorothymidine (F3TdR). We have called this...
Bromodeoxyuridine triphosphate is an allosteric inhibitor of ribonucleotide reductase, and bromodeoxyuridine can therefore kill cells by starving them for deoxycytidine nucleotides. The toxicity of bromodeoxyuridine for some cell lines is reduced many fold when deoxycytidine is also present. For...
IntroductionThis study aimed at clarifying the dynamics of bromodeoxyuridine (BrdU) label-retaining cells (LRCs) and their relationship to cell proliferation and apoptosis during pulpal healing after cavity preparation in mice.
The thymidine analog bromodeoxyuridine (BrdU) is incorporated into newly synthesized DNA and has been shown to increase the susceptibility of incorporating cells to ionizing radiation. However, in the absence of secondary stressors, BrdU is thought to substitute relatively benignly for thymidine...
Relative utilization of dThd, BrdUrd, and IdUrd as exogenous precursors of DNA in vivo was compared with utilization of the respective triphosphates in vitro. To measure relative utilization, exponentially growing P-815 or CHO cells were incubated with different mixtures of dThdBrdUrd or dThdIdU...
To explore new scaffolds for the treat of Alzheimer’s disease appears to be an inspiring goal. In this context, a series of varyingly substituted flavonols and 4-thioflavonols have been designed and synthesized efficiently. All the newly synthesized compounds were characterized unambiguously by...
Several new classes of hybrid catalysts have been synthesized by tethering heterocyclic metal (Lewis acid) chelating scaffolds to several different amines capable of facilitating enamine catalysis. Oxazole, thiazole, and imidazole-based chiral precatalysts were prepared in several steps from ami...
A series of novel diaziridinyl quinone isoxazole hybrids (9a-9j) were synthesized starting from 2, 5-dimethoxy acetophenone 1 via Claisen reaction, cyclisation, alkoxy carbonylation, hydrolysis, oxidation and aziridine insertion. All the compounds were screened for antimicrobial, anti-biofilm an...
RH1, 3-methyl-6-hydroxymethyl-2,5-diaziridinyl-1,4-benzoquinone, is a NQO1 (NAD(P)H quinone oxidoreductase) directed anti-tumor agent. It is designed as a water soluble analog of MeDZQ (3,6-dimethyl-2,5-diaziridinyl-1,4-benzoquinone) and is a drug candidate for clinical evaluation. A HPLC assay ...
Small molecule organic dyes (SMODs) FWD7 and FWD8 featuring novel donor bis(arylvinyl)phenyl amino (BAPA) were designed for dye-sensitized solar cells (DSSCs). Absorption spectra of FWD7 featuring furanyl groups and FWD8 featuring thiophenyl groups showed about 20 nm bathochromic shifts and obvi...
Electropolymerization of 3,5-bis(4-bromophenyl)dithieno[3,2-b;2′,3′-d]thiophene, having a mild electron-withdrawing bromine atom attached to the para position of the two phenyl groups of dithienothiophene, was performed, utilizing a potentiodynamic method. The resultant homopolymer was charact...
In this work, the magnetic amino-functionalized microporous organic network composites (Fe3O4@MON-NH2) were rational designed and facile synthesized for magnetic solid phase extraction (MSPE) of endocrine disrupting chemicals (EDCs), followed by their analysis with high-performance liquid chroma...
(2E)-1-(2,4-Dichlorophenyl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one is synthesized by using 2,4-dichloroacetophenone and 3,4,5-trimethoxybenzaldehyde in ethanol. The structure of the compound was confirmed by IR and single crystal X-ray diffraction studies. FT-IR spectrum of (2E)-1-(2,4-dichlo...
Ethyl 2-(4-bromophenyl)-1-(2,4-dichlorophenyl)-1H-4-imidazolecarboxylate (TG41) enhanced the binding both of γ-aminobutyric acid (GABA) and of flunitrazepam to rat cerebral cortical membranes. Electrophysiological recordings from Xenopus oocytes expressing various recombinant GABAA receptor sub...
The dehydration of cis- and trans-2-methylcyclopentanol on BPO catalysts with PB from 0.6 to 1.4, yields only 1-methylcyclopentene and 3-methylcyclopentene, with the relative amounts depending on the catalyst composition and the alcohol conformation. This data and that obtained from water-ad...
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