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Incorporation of a rigid 1,3-diketone-containing fragment led to significantly improved AXL inhibitory activity: design, synthesis, and SAR of the anilinopyrimidine AXL inhibitors.
Mol Divers
December 2024
Small-Molecule Drug Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai, 201203, People's Republic of China.
Overexpressed AXL kinase is involved in various human malignancies, which incurs tumor progression, poor prognosis, and drug resistance. Suppression of the aberrant AXL axis with genetic tools or small-molecule inhibitors has achieved valid antitumor efficacies in both preclinical studies and clinical antitumor campaigns. Herein we will report the design, synthesis, and structure-activity relationship (SAR) exploration of a series of anilinopyrimidine type II AXL inhibitors.
View Article and Find Full Text PDFHigh-Throughput Exploration of Ti-V-Nb-Mo Carbide MXenes Using Neural Network Potentials and Their Evaluation as Catalysts for Hydrogen Evolution Reaction.
ACS Appl Mater Interfaces
December 2024
TCS Research, Sahyadri Park 2, Rajiv Gandhi Infotech Park, Hinjewadi Phase 3, Pune 411057, India.
Realization of a sustainable hydrogen economy in the future requires the development of efficient and cost-effective catalysts for its production at scale. MXenes (MX) are a class of 2D materials with 'n' layers of carbon or nitrogen (X) interleaved by 'n+1' layers of transition metal (M) and have emerged as promising materials for various applications including catalysts for hydrogen evolution reaction (HER). Their properties are intimately related to both their composition and their atomic structure.
View Article and Find Full Text PDFSynthesis and molecular docking analysis of novel hydrazone and thiosemicarbazide derivatives incorporating a pyrimidine ring: exploring neuroprotective activity.
J Biomol Struct Dyn
December 2024
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Biruni University, Istanbul, Türkiye.
The increasing global prevalence of Alzheimer's disease necessitates the development of novel therapeutic approaches. Neurodegenerative diseases are associated with increased oxidative stress and levels of cholinesterase enzymes. Hence, the development of cholinesterase inhibitors and antioxidants may provide neuroprotective effects.
View Article and Find Full Text PDFTurkish version of the German Eating Behavior Scale (SEV-Tr): a study of reliability and construct validity.
Psychol Health Med
December 2024
Department of Nutrition and Dietetics, Faculty of Health Sciences, Hacettepe University, Ankara, Turkey.
This two-phase study aims to develop the Turkish version of the German Eating Behavior Scale (SEV-Tr), and to investigate the potential associations of eating behaviors with nutritional and health status. In the first phase, the original scale was adapted to the Turkish language and its validity and reliability were assessed in 299 healthy individuals aged 19-64 years. In the second phase, the SEV-Tr was retested in a study population of 110 healthy individuals, aged 19-64 years, and the potential associations between the SEV-Tr score, anthropometrical and biochemical measurements, and other eating behaviors assessed by the Three-Factor Eating Questionnaire (TFEQ-Tr21) were examined.
View Article and Find Full Text PDF<b>Background and Objective:</b> Cervical cancer is the second most common cancer in Indonesia, where traditional herbal treatments like <i>Zanthoxylum acanthopodium</i> (andaliman) are culturally used. Investigating protein biomarkers such as E7, pRb, EGFR and p16 can help assess the efficacy of these treatments. <b>Materials and Methods:</b> There were 5 groups in this study: 2 control groups (C- and C+) and 3 treatment groups (each receiving one of three doses).
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