Synthesis and Antitumor Activity of Fluorocyclopentenyl-Pyrimidines

Synthesis of fluorocyclopentenyl pyrimidine nucleosides 6–9 was enantiopurely accomplished employing oxidative rearrangement, RCM reaction and electrophilic fluorination starting from d-ribose. Cytosine analog 8 was found to exhibit significant anticancer activity in various human tumor cell lines.     

Effect of Elastic Network of Ceramic Fillers on Thermal Cycle Stability of a Solid Oxide Fuel Cell Stack

Glass‐based seals for planar solid‐oxide fuel‐cell (SOFC) stacks are open to uncontrolled deformation and mechanical damages, limiting both sealing integrity and stack reliability, particularly in thermal cycle operations. If the glass‐based seals work like an elastomer‐based compressive seal, SOFC stacks may survive unprecedented numbers of thermal cycles. A novel composite sealing gasket is successfully developed to mimic the unique features of the elastomer‐based compressive seal by controlling the composition and packing behavior of binary ceramic fillers. A single‐cell SOFC stack undergoes more than 100 thermal cycles with little performance loss, during which the sealing integrity is lost/recovered repeatedly upon cooling and reheating, corresponding to unloading/loading of the elastomer‐based compressive seal. The thermal‐cycle responses of the SOFC stack are explained in sequence by the concurrent events of elastic deformation/recovery of ceramic filler network and corresponding redistribution of sealing glass.     

First-order kinetics analysis of monomer composition dependent polyhydroxyalkanoic acid degradation in Pseudomonas spp

The intracellular degradation of polyhydroxyalkanoic acid (PHA) in pseudomonads was investigated by first-order kinetics analysis using the initial rate method. One type of PHA was accumulated in five Pseudomonas spp., P. oleovorans, P. aeruginosa, P. fluorescens, P. citronellolis, and P. putida, by growing them on octanoic acid. The monomer compositions of the five PHA were not significantly different from one another: 85-90 mol % 3-hydroxyoctanoic acid (3HO), 7-12 mol % 3-hydorxycaproic acid (3HC), and 3-6 mol % 3-hydroxydecanoic acid (3HD). The first-order degradation rate constants (k(1)) for the octanoate-derived PHA (designated P(3HO)) in the five species were in a similar range between 0.060 and 0.088 h(-1). This may indicate the similar specificities of the five intracellular depolymerases. In addition, the similar k(1) among the different species may correlate with the high degree of amino acid sequence identities (over 85%) among the intracellular PHA depolymerase phaZ genes. Six other chemically different types of PHA were accumulated in P. putida from n-nonanoic acid, n-decanoic acid, 5-phenyvaleric acid, or 11-phenoxyundecanoic acid as a single or a mixed carbon source. The calculated k(1) values were characteristic to each PHA, reflecting their chemical structures. In comparison with P(3HO), an increase in the levels of the two minor monomers 3HC and 3HD as in P(21 mol % 3HC-co-56 mol % 3HO-co-23 mol % 3HD) significantly slowed the rate of intracellular degradation. From the comparison of k(1) values, it is suggested that the P. putida intracellular depolymerase is most active against P(3HO).     

Synthesis and biological evaluation of quinoxaline-5,8-diones that inhibit vascular smooth muscle cell proliferation

A series of 6-arylamino-2,3-bis(pyridin-2-yl)-7-chloro-quinoxaline-5,8-diones were synthesized and evaluated for their inhibitory activity on the rat aortic smooth muscle cell (RAoSMC) proliferation. The quinoxaline-5,8-diones exhibited a potent antiproliferative activity. Further mechanistic study revealed that the inhibitory effect of one representative quinoxaline-5,8-dione on SMC proliferation was mediated by modulation of the extracellular signal-regulated kinase 1/2 signaling pathway in the RAoSMCs.