HGF/c-Met signaling has been implicated in human cancers. Herein we describe the invention of a series of novel triazolopyrazine c-Met inhibitors. The structure-activity relationship of these compounds was investigated, leading to the identification of compound 28, which demonstrated favorable pharmacokinetic properties in mice and good antitumor activities in the human glioma xenograft model in athymic nude mice.
An electronic density model was developed
and used to identify
a novel pyrrolotriazinone replacement for a quinazolinone, a commonly
used moiety to impart selectivity in inhibitors for PI3Kγ and
PI3Kδ. Guided by molecular docking, this new specificity piece
was then linked to the hinge-binding region of the inhibitor using
a novel cyclic moiety. Further structure–activity relationship
optimization around the hinge region led to the discovery of candidate 26, a highly potent and selective PI3Kγ–PI3Kδ
dual inhibitor with favorable drug metabolism and pharmacokinetic
properties in preclinical species.
In this paper, we present a novel dataset named MVB (Multi View Baggage) for baggage ReID task which has some essential differences from person ReID. The features of MVB are three-fold. First, MVB is the first publicly released large-scale dataset that contains 4519 baggage identities and 22660 annotated baggage images as well as its surface material labels. Second, all baggage images are captured by specially-designed multi-view camera system to handle pose variation and occlusion, in order to obtain the 3D information of baggage surface as complete as possible. Third, MVB has remarkable inter-class similarity and intra-class dissimilarity, considering the fact that baggage might have very similar appearance while the data is collected in two real airport environments, where imaging factors varies significantly from each other. Moreover, we proposed a merged Siamese network as baseline model and evaluated its performance. Experiments and case study are conducted on MVB.
High-speed press lines are related to the fierce competition in the automobile industry and rely on continuous high-efficiency automated feeding systems. Kinematic simulation systems have facilitated the improvement of production processes by generating real-time kinematic curves to avoid interference in feeding systems. In this article, a new method based on quintic polynomials in MATLAB and ADAMS is introduced to achieve whole-line planning using a kinematic simulation system for path planning. Furthermore, secondary interface is developed to visualize the kinematic curves and animate the generated whole-line trajectories. The kinematic simulation system was found to improve the efficiency of generating predicted trajectories in joint or Cartesian space and achieved reliable whole-line path planning, including collision inspection and singular point detection, by using parametric modeling and analyzing kinematic curves. Finally, the kinematic simulation system was verified using results of a kinematic analysis and example simulation.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.