SARS-CoV-2 M inhibitors with antiviral activity in a transgenic mouse model.

The COVID-19 pandemic caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) continually poses serious threats to global public health. The main protease (M) of SARS-CoV-2 plays a central role in viral replication. We designed and synthesized 32 new bicycloproline-containing M inhibitors derived from either boceprevir or telaprevir, both of which are approved antivirals.

Discovery of Potent and Selective Inhibitors of Cdc2-Like Kinase 1 (CLK1) as a New Class of Autophagy Inducers.

Autophagy inducers represent new promising agents for the treatment of a wide range of medical illnesses. However, safe autophagy inducers for clinical applications are lacking. Inhibition of cdc2-like kinase 1 (CLK1) was recently found to efficiently induce autophagy.

From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer.

Herein we report the sophisticated process of structural optimization toward a previously disclosed Src inhibitor, compound 1, which showed high potency in the treatment of triple negative breast cancer (TNBC) both in vitro and in vivo but had considerable toxicity. A series of 3-(phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine derivatives were synthesized. In vitro cell-based phenotypic screening together with in vivo assays and structure-activity relationship (SAR) studies finally led to the discovery of N-(3-((4-amino-1-(trans-4-hydroxycyclohexyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)ethynyl)-4-methylphenyl)-4-methyl-3-(trifluoromethyl)benzamide (13an).

[A new method for predicting anterior chamber depth in intraocular lens implantation].

Objective: To propose a method for predicting the postoperative anterior chamber depth value (ACD) based on the evaluation standard of contrast sensitivity function (CSF).

Methods: In a personalized eye model, the natural lens was replaced with an artificial lens, and the tracing method based on ZEMAX software was utilized to simulate the pseudophakic optical system. The best MTF curve was obtained through optical optimization to calculate the CSF and determine the best contrast sensitivity (CS) curve.

[Two-step image registration based on control volumes].

Objective: To increase the accuracy of beam targeting and improve the dose distributions in radiotherapy using a robust image registration algorithm based on control volumes.

Methods: Control volume mapping and thin-plate spline deformable transformation were combined. The use of the control volumes increased the accuracy for the deformable registration.

[Application of 3D FIESTA sequence in magnetic resonance sialography for obstructive salivary diseases].

Objective: To investigate the value of 3D FIESTA sequence in magnetic resonance sialography (MRS) in the diagnosis of obstructive salivary diseases.

Methods: Eleven patients with obstructive salivary diseases underwent MRS, and three-dimensional (3D) reconstruction and virtual endoscopic images of the salivary gland ducts were obtained after MRS data post-processing for comparison with those of sialoendoscopy.

Results: The diagnostic accuracy of MRS was 72.

[Magnetic resonance imaging of bone and joint transfixed with stainless steel lag screws].

To explore the method of displaying the bone and joint structures transfixed with stainless steel lag screws using magnetic resonance imaging (MRI), 2 patients whose knee joints (and ankle joint in one case) were transfixed with stainless steel underwent MRI with FSE-XL pulse sequence. The images clearly displayed the bones, ligaments and articular cartilage around the stainless steel materials, demonstrating the efficacy of FSE-XL pulse sequence in evaluation of the anatomical features of the bones and joints transfixed with stainless steel materials.

[Nonlinear analysis of epileptic multichannel EEG].

Objective: To study the difference between the nonlinear eigenvalue of epileptic patients and normal subjects for accurate identification of epileptic EEG signal.

Methods: Multivariable phase space reconstruction technique was employed to analyze the EEG of epileptic patients for estimating the correlation dimension(D(2)), which was one of the most often used parameters in quantitative discretion of complicated nonlinear dynamics system.

Result And Conclusion: The correlation dimension is an important eigenvalue for epileptic EEG identification.

[Design of the medical record database of diabetes mellitus].

The system requirement of the clinical record database of diabetes mellitus was analyzed, the functional module built and the design scheme established on the basis of the general design objective for a distributed database with distributed objects.

[Study of fuzzy analytical system for physiological signals during sleep].

A new approach to sleep analysis based on fuzzy prediction theory is described. This article gives a general introduction to detection and processing of biologic signals with LabVIEW software, and the application of the designed fuzzy measurement system in fuzzy prediction analysis of the physiological signals recorded during sleep. The results of trials of the fuzzy prediction analysis demonstrated the reliability of this method.

[Evaluation method of CT number linearity].

Objective: To explore the method for computed tomography (CT) number linearity evaluation.

Methods: The model CTP401 of Catphan500 phantom was adopted to test 43 sets of CT scanners under the same scanning conditions. 1- and 2-order curve fitting of the testing results of each scanner were performed, with the bending of the 2-order fitted curve defined as the degree of CT number non-linearity and the slope of the linear fitting as contrast scale.