A5090756918- Cancer-related Molecular Pathways
- Chemical Synthesis and Analysis
- DNA and Nucleic Acid Chemistry
- Advanced Breast Cancer Therapies
- Video Surveillance and Tracking Methods
- Click Chemistry and Applications
- Biochemical and Molecular Research
- Cancer Mechanisms and Therapy
- Microtubule and mitosis dynamics
- Pharmacogenetics and Drug Metabolism
- Advanced Neural Network Applications
- Synthesis and Characterization of Heterocyclic Compounds
- Chemical Reactions and Isotopes
- Angiogenesis and VEGF in Cancer
- Cancer therapeutics and mechanisms
- Adenosine and Purinergic Signaling
- Ionosphere and magnetosphere dynamics
- Human Pose and Action Recognition
- Fluorine in Organic Chemistry
- Analytical Chemistry and Chromatography
- Catalytic C–H Functionalization Methods
- Solar and Space Plasma Dynamics
- Diabetes Treatment and Management
- HIV/AIDS drug development and treatment
- Carbohydrate Chemistry and Synthesis
Johnson & Johnson (United States)
2006-2024
Janssen (United States)
2012-2024
Fujian Medical University
2024
Fujian Provincial Cancer Hospital
2024
China People's Public Security University
2023-2024
Springhouse
2017-2020
Janssen (Belgium)
2014
Molecular Oncology (United States)
2002
University of California, Berkeley
1998-1999
Southern Illinois University Carbondale
1996-1998
A series of 1-acyl-1H-[1,2,4]triazole-3,5-diamine analogues were synthesized as cyclin-dependent kinase (CDK) inhibitors. These compounds showed potent and selective CDK1 CDK2 inhibitory activities inhibited in vitro cellular proliferation various human tumor cells. Representative compound 3b demonstrated vivo efficacy a melanoma A375 xenograft model nude mice.
Modulation of aberrant cell cycle regulation is a potential therapeutic strategy applicable to wide range tumor types. JNJ-7706621 novel inhibitor that showed potent inhibition several cyclin-dependent kinases (CDK) and Aurora selectively blocked proliferation cells various origins but was about 10-fold less effective at inhibiting normal human growth in vitro. In cancer cells, treatment with inhibited independent p53, retinoblastoma, or P-glycoprotein status; activated apoptosis; reduced...
Canagliflozin is an oral antihyperglycemic agent used for the treatment of type 2 diabetes mellitus. It blocks reabsorption glucose in proximal renal tubule by inhibiting sodium-glucose cotransporter 2. This article describes vivo biotransformation and disposition canagliflozin after a single dose [<sup>14</sup>C]canagliflozin to intact bile duct-cannulated (BDC) mice rats dogs humans. Fecal excretion was primary route elimination drug-derived radioactivity both animals In BDC rats, most...
Natural (−)-cocaine and unnatural (+)-cocaine have been synthesized enantiospecifically from d- l-glutamic acid, respectively. The axial−equatorial substitutents were introduced by a stereo- regiospecific dipolar cycloaddition to the corresponding (1R,5S)- (1S,5R)-N-BOC-nortropenes with (ethoxycarbonyl)formonitrile N-oxide. A sequence of subsequent stereochemically controlled transformations converted fused isoxazoline requisite β-hydroxy ester. Synthesis key intermediate N-BOC-nortropenes...
In this case study we report a substorm, 23 March 2007, which exhibited oscillations with period of ∼135 s in three substorm phenomena all were one‐to‐one correlated. The in‐situ observations are from one THEMIS spacecraft (8.3 R E geocentric distance) and the geosynchronous LANL‐97A spacecraft. focus here is on intensification phase during was conjugate to region auroral brightening its foot point near high‐latitude ground station Kiana. following results will be demonstrated: (1)...
Abstract Infections with intestinal worms, such as Ascaris lumbricoides, affect hundreds of millions people in all tropical and subtropical regions the world. Through large-scale deworming programs, World Health Organization aims to reduce moderate-to-heavy intensity infections below 1%. Current diagnosis monitoring these control programs are solely based on detection worm eggs stool. Here we describe how metabolome analysis was used identify A. lumbricoides -specific urine biomarker...
We report a new strategy for the enantiospecific synthesis of (R)-4-amino-5-oxo-1,3,4,5-tetrahydrobenz[cd]indole. This compound is an advanced intermediate which contains tricyclic core many tetracyclic ergot alkaloids. Our method involves initial D-4-bromotryptophan from coupling indolyllithium species with masked serinal. The alpha-amino position was protected N-trityl group, ensuring enantiomeric integrity this during ensuing organometallic cyclization reaction. Stabilization tricycle...
We report the combination of organo-photocatalysis with transition metal (TM) catalysis for directed ortho-hydroxylation substituted anilides synthesis α-aminophenol derivatives under mild conditions. The developed metallaphotocatalysis utilizes N-pivaloyl as a directing group and phenyl iodine(III) bis(trifluoroacetate) (PIFA) in 1,2,3,5-tetrakis(carbazol-9-yl)-4,6-dicyanobenzene (4CzIPN) photocatalyst [RuCl2(p-cymene)]2 TM catalyst visible-light irradiation at room temperature....
Abstract Stable isotope‐labeled ([ 13 C 2 , D 3 ]) and carbon 14‐labeled vasopressin receptor antagonist RWJ‐676070, a spirobenzazepine amide, were prepared in separate syntheses for use drug metabolism studies. The stable isotopically labeled sample was starting from [ 6 ]dimethyl sulfate C]copper (I) cyanide nine steps with 14% overall isotopic yield. 14 label introduced five C]potassium to provide material having specific activity of 58 mCi/mmol (2.15 GBq/mmol). Selective hydrolysis the...
Person re-identification is a technology used to identify individuals across different cameras. Existing methods involve extracting features from an input image and using single feature for matching. However, these often provide biased description of the person. To address this limitation, paper introduces new method called Dual Descriptor Feature Enhancement (DDFE) network, which aims emulate multi-perspective observation abilities humans. The DDFE network uses two independent sub-networks...
During the anomalously low density solar wind interval of May 1999, GEOTAIL was in magnetosheath for ∼37 hours after making an inbound crossing expanding bow shock at ∼8 R E upstream its nominal position. Comparison among data sets obtained from (magnetosheath), WIND (near upstream‐bow shock), and ACE (far upstream) reveals several unique features: Firstly, during 1430–1530 UT on 11 May, we observed both double‐peaked protons with a peak separation 250–300 km/s, which close to local Alfvén...
To address challenges related to the inadequate representation and inaccurate discrimination of pedestrian attributes, we propose a novel method for person re-identification, which leverages global feature learning classification optimization. Specifically, this approach integrates Normalization-based Channel Attention Module into fundamental ResNet50 backbone, utilizing scaling factor prioritize enhance key information. Furthermore, dynamic activation functions are employed adaptively...
In order to minimize the disparity between visible and infrared modalities enhance pedestrian feature representation, a cross-modality person re-identification method is proposed, which integrates modality generation enhancement. Specifically, lightweight network used for dimension reduction augmentation of images, intermediate are generated bridge gap images images. The Convolutional Block Attention Module embedded into ResNet50 backbone selectively emphasize key features sequentially from...
New medications are needed to improve outcomes of castration-resistant prostate cancer (CRPC). Psoralen has been reported have anti-cancer properties for various tumors, but there limited reports about psoralen treatment in (PCa). This study aimed investigate the effect on PC3 cells and potential underlying mechanisms action.
The oxidation selectivity of the η6-arene ligand in a series [(η5-C5Me5)Ir(η6-arene)](OTf)2 complexes to corresponding [(η5-C5Me5)Ir(η5-phenoxo)](OTf) derivatives was studied as complementary protocol metal-catalyzed borylation-oxidation. A representative compounds prepared with mono-, di-, and trisubstituted arenes well two examples biphenyls rationally explore site C(sp2)–H oxidation. isolated organometallic arene were treated NaClO2 formed desired iridium η5-phenoxo products. While...
Abstract ROESY and NOESY NMR spectroscopic analyses of the ribofuranosyl (1a), 2′-deoxyribofuranosyl (1b), arabinofuranosyl (1c) derivatives 6-formyluracil in (CD3)2SO D2O solutions have established that each exclusive 7,05′-cyclic hemiacetal diastereomer 1a,b major 7,O2′-cyclic 1c possess 7R configuration. In addition, (7R)-1c has been shown to be thermodynamically more stable than (7S)-1c, contrary our previous indication. A new, higher yielding synthetic route 1a developed, 1b obtained...