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N-Acyl-2-aminothiazoles with nonaromatic acyl side chains containing a basic amine were found to be potent, selective inhibitors of CDK2/cycE which exhibit antitumor activity in mice. In particular, compound 21 [N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4-piperidinecarboxamide, BMS-387032], has been identified as an ATP-competitive(More)
High throughput screening identified 2-acetamido-thiazolylthio acetic ester 1 as an inhibitor of cyclin-dependent kinase 2 (CDK2). Because this compound is inactive in cells and unstable in plasma, we have stabilized it to metabolic hydrolysis by replacing the ester moiety with a 5-ethyl-substituted oxazole as in compound 14. Combinatorial and parallel(More)
Synthesis and SAR of substituted pyrrolotriazine-4-one analogues as Eg5 inhibitors are described. Many of these analogues displayed potent inhibitory activities in the Eg5 ATPase and A2780 cell proliferation assays. In addition, pyrrolotriazine-4-one analogue 26 demonstrated in vivo efficacy in an iv P388 murine leukemia model. Both NMR and X-ray(More)
High-throughput screening of a subset of the J&J compound library containing the carboxylic acid functional group uncovered a bromophenyl derivative as a moderate potent GPR40 agonist. Chemical elaboration of this bromophenyl led to the discovery of a novel series of GPR40 agonists with submicromolar potency. Among them, 22 and 24 behaved as full agonists(More)
Keywords: Hydrothermal power systems Economic load scheduling Combined economic emission scheduling Quantum-behaved particle swarm optimization a b s t r a c t This paper presents an improved quantum-behaved particle swarm optimization (IQPSO) for short-term combined economic emission hydrothermal scheduling, which is formulated as a bi-objective problem:(More)
In this paper we describe a new approach to distinguish and extract text from images with various objects and complex backgrounds. The goal of our approach is to present characters in images with clear background and without other objects. The proposed approach mainly includes two steps. Firstly, a density-based clustering method is employed to segment(More)
We study the quantum version of a decision tree classifier to fill the gap between quantum computation and machine learning. The quantum entropy impurity criterion which is used to determine which node should be split is presented in the paper. By using the quantum fidelity measure between two quantum states, we cluster the training data into subclasses so(More)
Based on the previous introduced quantum-behaved particle swarm optimization (QPSO), in this paper, a revised novel QPSO with hybrid cooperative search is proposed. Taking full advantages of the characteristics of mutualism among swarms, the cooperative search is carried out to improve the diversity of the swarms, so as to help the system escape from local(More)