The title compounds (2E)-1-(4-2,4-dichlorophenyl)-3-[4-(propan-2-yl)phenyl]prop-2-en-1-one (I) and 2E)-1-(4-fluorophenyl)-3-[4-(propan-2-yl) phenyl]prop-2-en-1-one (II), have been synthesized by the base catalyzed Claisen-Schmidt condensation reaction of 4-(propan-2-yl)benzaldehyde with substitu...

BackgroundThe objectives were to describe morbidity and mortality after tricuspid valve (TV) surgery, to compare outcomes after repair versus replacement, and to assess risk factors for mortality and tricuspid regurgitation (TR) recurrence.

The vertical excitation energies for the low-lying singlet excited states of the HfO2 molecule were calculated at the SAC-CI/aug-cc-pVTZ-PP level, and were compared with those of ZrO2 and TiO2. The ground electronic state (X1A1) and ten selected singlet excited states (21A1, 31A1, 11A2, 21A2, 11...

Contribution of the ABCB1/MDR1/P-glycoprotein drug transporter to breast cancer resistance has been controversial. One issue is that ABCB1-dependent drug-resistance has primarily been investigated in mammary epithelial cell models technically manipulated to overexpress ABCB1, either by gene tran...

SummaryBackgroundThis phase 1, dose-finding study determined the safety, maximum tolerated dose (MTD)/recommended phase 2 dose (RP2D), antitumor activity, and molecular correlates of IPI-926, a Hedgehog pathway (HhP) inhibitor, combined with cetuximab in patients with relapsed/metastatic squamou...

The Hylleraas-CI (Hy-CI) method is conventionally defined as based on superposition-of-configurations (also called configuration interaction) wave functions in which each term (configuration) is built from an orbital product to which is appended at most one linear factor rij, where rij is the di...

The promnesic effects of RU 35 926 (CI-979), a muscarinic receptor agonist, were evaluated on memory impairments induced by the muscarinic antagonist scopolamine, using a radial arm maze task, in comparison with tetrahydroaminoacridine (THA), a cholinesterase inhibitor. Groups of rats were train...

Inflammatory mediators of the arachidonic acid cascade from cyclooxygenase (COX) and lipoxygenase (LOX) pathways are primarily responsible for many diseases in human beings. Chronic inflammation is associated with the pathogenesis and progression of cancer, arthritis, autoimmune, cardiovascular ...

Three series of aza-caffeic acid derivatives with different linkers were designed and synthesized. Each of the synthesized derivatives was then used in cytotoxicity screening on either 8 or 12 human cancer cell lines. The structure–activity relationships on three structural regions A, B, and C ...

Cyclooxygenase-2 is a very important physiological enzyme playing key roles in various biological functions especially in the mechanism of pain and inflammation, among other roles, making it a molecule of high interest to the pharmaceutical community as a target. COX 2 enzyme is induced only dur...

In this study, we report the design and synthesis of novel hybrids of caffeic acid phenetyl ester (CAPE) and non-steroidal anti-inflammatory drugs (NSAIDs). We assessed their effects on an experimental ocular inflammation in New Zealand rabbits. The formulations of CAPE–aspirin and CAPE–indome...

In this detailed study of the photoreaction of 2,5-bis(dibenzylamino)-3,6-dichloro-p-benzoquinone, two new products were separated along with the previously reported debenzylated analogues, and their molecular structure was determined. One compound was identified as 2-(benzylamino)-3,6-dichloro-...

Two analogous positional polymers P16PySO and P27PySO have been synthesized via the copolymerization from dibenzothiophene-S,S-dioxide and pyrene building blocks. The effect of the linking pattern on the molecular packing, photophysical and photocatalytic properties of the two isomers was invest...

A synthesis of (1R,2S)-dehydrocoronamic acid ethyl ester was developed employing a regio- and enantioselective palladium-catalysed nucleophilic ring-opening of 3,4-epoxy-1-butene with a glycine anion equivalent as the key enantiodifferentiating step. The desired selectivity was achieved using Tr...

A systematic rationalization of the hundreds of proteins harboring iron-sulfur clusters and able to exhibit the most diverse biological functions is missing. In this picture we have already reviewed structure/electrochemistry of metalloproteins expressing single types of iron-sulfur centres [nam...

CPT-11 is a first-line chemotherapy for advanced or metastatic colorectal cancers. 7-Ethyl-10-hydroxycamptothecin (SN38), the active metabolite of CPT-11, has an anticancer efficacy 100–1000 folds more than CPT-11 in vitro. However, the drawbacks such as ultralow solubility and poor stability, ...

OSU-2S is a novel anti-cancer and immune modulatory agent designed specifically to avert the immunosuppressive effects and related toxicities observed in clinical studies with its predecessor analog, FTY720. To characterize its preclinical pharmacokinetics, a liquid chromatography–tandem mass s...

An environmental friendly process to selectively acetylate primary alcohols was demonstrated. The esterification process consists of treatment of a primary alcohol in the presence of immobilized C. antarctica lipase (Novozyme-435) in ethyl acetate at room temperature. Primary alcohols were acety...

Daptomycin is a highly effective lipopeptide antibiotic against Gram-positive pathogens. The presence of (2S, 3R) 3-methyl glutamic acid (mGlu) in daptomycin has been found to be important to the antibacterial activity. However the role of (2S, 3R) mGlu is yet to be revealed. Herein, we reported...

The purpose of this study is to present defense R&D governance model for governance analysis and decision making in defense R&D programs. In particular, by utilizing the MIT Sloan IT governance matrix and through Delphi surveys of a group of defense R&D experts, an efficient governance model of ...