Novel Pan-Pim Kinase Inhibitors With Imidazopyridazine and Thiazolidinedione Structure Exert Potent Antitumor Activities.

Pim kinases are overexpressed in various types of hematological malignancies and solid carcinomas, and promote cell proliferation and survival. Here in this study, we investigated the preclinical profile of novel pan-Pim kinase inhibitors with imidazopyridazine and thiazolidinedione structure. Imidazopyridazine-thiazolidinediones inhibited activities of Pim kinases with IC values of tens to hundreds nanomolar.

Experiments of three identical huts with shape-stabilized phase change materials and simulation of detached house in Japanese climate classification.

The data in this article are the experiment and simulation results of three identical huts were examined using by using varying shape-stabilized PCMs (SSPCMs) sheet levels in winter of Chiba prefecture where Japanese temperate climate. A shape-stabilized phase-change material (SSPCM) established the melting- and solidification-temperature ranges at 19-26 °C was installed on the floor, walls, and ceiling of various buildings, and its effects on indoor room temperature stabilization and heating load reduction were examined using experiments and simulations. The PCM model was developed based on the specific heat capacity measured using a thermostatic chamber and simulations results were obtained using EnergyPlus.

Data on experiments result of three identical huts with shape-stabilized phase change materials in Japanese temperate climate.

The data in this article are the experimental results of three identical huts (Hut A, B and C), which were examined by using varying shape-stabilized PCMs (SSPCMs) sheet levels under natural and heating conditions in winter of Chiba prefecture where Japanese temperate climate. The SSPCMs sheet established the melting and solidification-temperature ranged at 19-26 °C were used. In Hut A, no SSPCM sheets were applied; in Hut B, four layers of SSPCM sheets were applied to the floor; in Hut C, one layer of SSPCM was applied to the floor, walls, and ceilings.

Rational Design of a Potent Pan-Pim Kinases Inhibitor with a Rhodanine-Benzoimidazole Structure.

Background/aim: The serine/threonine Pim kinases are overexpressed in various types of solid carcinomas and hematological malignancies, and contribute to regulating cell-cycle progression and cell survival. The aim of this study was to discover a novel pan-Pim kinases inhibitor with potent anti-proliferative activities against cancer cell lines.

Materials And Methods: We screened a panel of small molecule compounds for their ability to inhibit Pim-1 kinase activity, and the hit compound was optimized using the docking analysis to Pim-1.

Data on anti-insulation detection via Point of Thermal Inflexion (PTI) in 1248 cases; 13 climates, four occupancy profiles, six wall configurations and four insulation levels.

The data in this article are the simulation results of 1248 cases that were carried out to detect anti-insulation behaviour in the article titled "Anti-insulation mitigation by altering the envelope layers' configuration" (Idris and Mae, 2017) [1]. These cases are generated by a matrix of 13 climates, 6 envelope layer configurations, 4 occupancy profiles and 4 levels of insulation thickness. The data are concerned with the annual cooling and heating loads of these cases.

Highly regioselective synthesis of gem-difluoroallenes through magnesium organocuprate SN2' substitution.

[reaction: see text]. The reaction of gem-difluoropropargyl electrophiles with Grignard reagents is complicated by the inherent difficulty of executing nucleophilic substitutions on a CF2 group, and the facile formation of carbenoid intermediates arising from alpha-elimination of fluoride. In the presence of an excess amount of a copper salt, a Grignard reagent reacts with gem-difluoropropargyl bromide via an S(N)2' mechanism to produce gem-difluoroallene in high yield.

Catalytic route to the synthesis of optically active beta,beta-difluoroglutamic acid and beta,beta-difluoroproline derivatives.

Beta,beta-difluorinated amino acid derivatives were synthesized via Mg(0)-promoted defluorination of alpha-trifluoromethyl iminoester. Bromination of the difluoroenamine afforded the bromodifluoromethyl iminoester in good yield. Pd-catalyzed asymmetric hydrogenation of the bromodifluoromethyl iminoester and the subsequent transformations provided optically active beta,beta-difluoroglutamic acid and beta,beta-difluoroproline derivatives.