Synthesis of trans-fused polycyclic ethers with angular methyl groups using sulfonyl-stabilized oxiranyl anions

An efficient method has been developed for the synthesis of trans-fused tetrahydropyrans with angular methyl groups adjacent to the ring oxygen. The procedure involves the coupling reaction of a sulfonyl-stabilized oxiranyl anion with an appropriate triflate followed by 6-endo cyclization, and is effective for the construction of 6/6- and 6/7/6-cyclic ether ring systems with sterically congested 1,3-diaxial methyl groups.     

Effect of a Combined Exercise and Cognitive Activity Intervention on Cognitive Function in Community-dwelling Older Adults: A Pilot Randomized Controlled Trial

Objective: The purpose of this study is to investigate the effect of an intervention combining exercise and cognitive activity on cognitive function in healthy older adults. Methods: This pilot randomized controlled trial recruited 33 eligible, healthy communitydwelling older adults (mean age, 77.1 years old; women, 51.5%), who were divided into intervention and waitlist control groups. The intervention group was engaged weekly in a group activity comprising exercise and discussions of homework, which included reading aloud, simple arithmetic, and simple activities, like spotting differences, for cognitive stimulation. They were also required to complete cognitive activity homework twice a week. The waitlist control group received no intervention. The main outcomes were cognitive function assessed using the Mini-Mental State Examination, delayed recall score on the Logical Memory IIA of the Wechsler Memory Scale Revised, Trail Making Test, and digit symbol substitution test. Results: According to the results, Mini-Mental State Examination scores were maintained in the intervention group but declined in the control group [Mean change in outcomes in control group (95% confidence interval): -1.68 (-2.89 to -0.48)]. Additional mean change in outcomes in intervention group were found [1.68 (0.02 to 3.35)]. Conclusions: Interventions combining exercise and cognitive activity can be helpful for preserving cognitive function in healthy older adults.     

Efficient functional molecule incorporation method to functionalized peptide nucleic acid (PNA): use in synthesis of labeled PNA oligomers

A novel efficient synthetic method for a functionalized PNA (peptide nucleic acid) is described, in which a functional molecule is incorporated in place of a nucleobase. Novel ω-AA-^BocPNA-OH (20-24, AA=amino acid) were designed as PNA precursor monomer units into which functional molecules could be incorporated efficiently. Compounds 20-24 reacted quantitatively with OSu (N-hydroxysuccinimidyl) active ester derivatives and isothiocyanate derivatives of commercial functional molecules to give target functionalized PNA monomer units 25-53. Various types of functionalized PNA monomer units could be efficiently incorporated into multiple predetermined positions in a PNA oligomer by SPPS (solid phase peptide synthesis) in the same way as for the four A(Cbz), G(Cbz), C(Cbz), and T PNA monomer units.     

Hysteresis and ferroelectric liquid crystal displays

One cause of the hysteresis in the voltage-transmittance curve is polarization in the alignment layers brought about by the spontaneous polarization of FLC molecules. The hysteresis was reduced by increasing the conductivity of the alignment layers. The structural changes on switching were examined by measuring time-resolved shifts of FT-IR peaks of selected groups. The shifts of selected groups in the IR peak can be attributed to changes in the local dielectric constants of the ambient environment during switching by molecular orbital calculations. The orientation on switching in the SmC* phase was found to be similar to that in the N* phase.     

Polymerization of Methyl Methacrylate with Samarocene Complex Supported on Mesoporous Silica

Synthesis of polymers with controlled molecular weight and narrow polydispersity is of both fundamental interest and practical importance. In recent years, high molecular weight poly (methyl methacrylate) (PMMA) having an unusually narrow polydispersity has been synthesized by using the unique initiating property of (C5Me5)2LnⅢR (R=H, Me, Ln=Sm, Yb) complexes1,2. Herein we report the results of the first example of the polymerization of methyl methacrylate (MMA) with samarocene complex …     

Pin1 and Par14 peptidyl prolyl isomerase inhibitors block cell proliferation

Disruption of the parvulin family peptidyl prolyl isomerase (PPIase) Pin1 gene delays reentry into the cell cycle when quiescent primary mouse embryo fibroblasts are stimulated with serum. Since Pin1 regulates cell cycle progression, a Pin1 inhibitor would be expected to block cell proliferation. To identify such inhibitors, we screened a chemical compound library for molecules that inhibited human Pin1 PPIase activity in vitro. We found a set of compounds that inhibited Pin1 PPIase activity in vitro with low microM IC50s and inhibited the growth of several cancer lines. Among the inhibitors, PiB, diethyl-1,3,6,8-tetrahydro-1,3,6,8-tetraoxobenzo[lmn] phenanthroline-2,7-diacetate ethyl 1,3,6,8-tetrahydro-1,3,6,8-tetraoxo-benzo[lmn] phenanthroline-(2H,7H)-diacetate, had the least nonspecific toxicity. These results suggest that Pin1 inhibitors could be used as a novel type of anticancer drug that acts by blocking cell cycle progression.