D-type cyclin-dependent kinase activities have not so far been detected in mammalian cells. Lysis of rodent fibroblasts, mouse macrophages, or myeloid cells with Tween 20 followed by precipitation antibodies to cyclins D1, D2, and D3 their major catalytic partner, 4 (cdk4), yielded immune complexes which readily phosphorylated the retinoblastoma protein (pRb) but histone H1 casein. Virtually all cyclin D1-dependent activity proliferating macrophages fibroblasts could be attributed cdk4. When...

Development of a stable nitroxyl radical class catalysts, 2-azaadamantane N-oxyl (AZADO) and 1-Me-AZADO, for highly efficient oxidation alcohols is described. AZADO 1-Me-AZADO exhibit superior catalytic proficiency to TEMPO, converting various sterically hindered the corresponding carbonyl compounds in excellent yields.

Abstract Curcumin (diferuloylmethane) is a dietary phytochemical with low toxicity that exhibits growth-suppressive activity against variety of cancer cells and possesses certain chemopreventive properties. has already been the subject several clinical trials for use as treatment in human cancers. Synthetic chemical modifications curcumin have studied intensively an attempt to find molecule similar but enhanced properties curcumin. In this study, series novel analogues were synthesized...

By using Southern blot analysis, we found that in two cases of human glioblastoma multiforme, cells carried amplified c-erbB genes which bore short deletion mutations within the ligand-binding domain epidermal growth factor (EGF) receptor. The products these mutated were about 30 kilodalton (kDa) smaller than normal 170-kDa EGF receptor, and tumor cell membrane fractions containing 140-kDa abnormal receptor showed a significant elevation tyrosine kinase activity without its ligand. In view...

5-Fluoro-2-azaadamantane N-oxyl (5-F-AZADO) realizes a simple, organocatalytic aerobic alcohol oxidation system that has wide scope under mild conditions at ambient pressure and temperature is weakly acidic halogen- transition-metal-free. The oxoammonium nitrate (5-F-AZADO+NO3−) works as bifunctional catalyst of 5-F-AZADO NOx enables the catalytic alcohols by itself (a metal-salt-free system).

To elucidate the pathogenesis of thyroid gland hypervascularity in patients with Graves' disease, we studied expression mRNAs for vascular endothelial growth factor (VEGF) and its receptor, Flt family, using human follicles vitro thiouracil-fed rats vivo. Human follicles, cultured absence cells, secreted de novo-synthesized hormone response to thyroid-stimulating (TSH) IgG. The produced VEGF mRNA but not flt-1 mRNA. was enhanced by insulin, tumor-promoting phorbol ester, calcium ionophore,...

Abstract The direct oxidation of unprotected amino alcohols to their corresponding carbonyl compounds has often posed serious challenges in organic synthesis and constrained chemists adopting an indirect route, such as a protection/deprotection strategy, attain goal. Described herein is highly chemoselective aerobic which 2‐azaadamantane N‐oxyl (AZADO)/copper catalysis used. catalytic system developed leads the alcohol‐selective various alcohols, carrying primary, secondary, or tertiary...

HA1077, but not the potent calcium entry blocker nicardipine reversed experimental chronic cerebral vasospasm induced in a two-hemorrhage canine model. The i.a. administration of HA1077 produced significant increases vertebral blood flow dogs. effects on vascular responses were studied vitro. Spiral strips rabbit aorta mounted for isometric tension recording physiological salt solution. competitive inhibition Ca++-induced contraction depolarized aorta. pA2 Ca@-induced was 6.71. inhibitory...

The in vitro and vivo vasorelaxant effects of HA1077, 1-(5-isoquinolinesulphonyl)-homopiperazine HCl, a novel vasodilator were examined. inhibitory HA1077 on contractile responses to various agonists examined strips rabbit aorta. concentration-response curves 5-hydroxytryptamine, prostaglandin F2alpha, histamine, angiotensin II, noradrenaline dopamine concentration-dependently shifted the right presence (0.3-3.0 microM). constant-pressure autoperfused coronary vascular bed dogs....

Practical and highly efficient methods for oxidative rearrangement of tertiary allylic alcohols to β-substituted α,β-unsaturated carbonyl compounds employing oxoammonium salts are described. The developed applicable acyclic substrates as well medium membered ring macrocyclic substrates. counteranion the salt plays crucial roles on this rearrangement.

A practical, three-step synthetic route to 9-azabicyclo[3.3.1]nonane N-oxyl (ABNO, 3), an unhindered, stable class of nitroxyl radical, has been developed. ABNO exhibits a highly active nature compared with TEMPO in the catalytic oxidation alcohols their corresponding carbonyl compounds.

Three of 16 human gastric adenocarcinoma samples, maintained as solid tumors in nude mice, were found to carry amplified c-myc genes. In two samples with a high degree DNA amplification (15- 30-fold), double minute chromosomes observed karyotype analysis. The level RNA was markedly elevated rapidly growing and poorly differentiated tumor, whereas it only slightly slowly more tumor.

A facile, green, one-pot oxidation of primary alcohols to carboxylic acids with broad substrate applicability has been developed by employing an expedient catalytic system consisting 1-Me-AZADO+X−/NaClO2.

A nitroxyl-radical-catalyzed oxidation of alcohols using diisopropyl azodicarboxylate (DIAD) as the terminal oxidant is reported. variety primary and secondary including aliphatic, benzylic, allylic are efficiently oxidized to their corresponding aldehydes ketones without overoxidation carboxylic acid. 1,2-Diols hydroxyl or diketones depending on amount DIAD used.

A highly active organocatalyst for alcohol oxidation has been developed. 9-Azanoradamantane N-oxyl (Nor-AZADO 4), constituting an unhindered, stable nitroxyl radical, exhibits superior catalytic activity to 2,2,6,6-tetramethylpiperidine-1-oxyl (TEMPO) and AZADOs in the of alcohols their corresponding carbonyl compounds.

A versatile, highly enantiocontrolled entry to the spiro-β-lactam core of chartellines has been developed by expanding scope oxidative nitrogen atom transfer methodology based on chiral Rh-nitrenoid species.

A highly enantioselective organocatalytic oxidative kinetic resolution (OKR) of racemic secondary alcohols has been accomplished using asymmetric organocatalysis. panel chirally modified 2-azaadamantane N-oxyls (AZADOs) exhibit superior catalytic activity and high enantioselectivity, allowing us to obtain optically active with a k(rel) value up 82.2.

The biochemical and pharmacological activities of nobiletin, including neurotrophic memory-enhancing action, in both vitro vivo systems are well established. However, whether its metabolites do have such beneficial effects like nobiletin remains to be examined. Here we, for the first time, report that 2-(4-hydroxy-3-methoxyphenyl)-5,6,7,8-tetramethoxychromen-4-one (4′-demethylnobiletin), a major metabolite identified urine rats mice, stimulates phosphorylation ERK CREB enhances CRE-mediated...

The development and characterization of enantioselective organocatalytic oxidative kinetic resolution (OKR) racemic secondary alcohols using chiral alkoxyamines as precatalysts are described. A number have been synthesized, their structure-enantioselectivity correlation study in OKR has led us to identify a promising precatalyst, namely, 7-benzyl-3-n-butyl-4-oxa-5-azahomoadamantane, which affords various aliphatic (ee up >99%, k(rel) 296). In mechanistic study, chlorine-containing...