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Pharmacological and structural insights into nanvuranlat, a selective LAT1 (SLC7A5) inhibitor, and its N-acetyl metabolite with implications for cancer therapy.
Sci Rep
January 2025
Department of Bio-System Pharmacology, Graduate School of Medicine, Osaka University, 2-2, Yamadaoka, Suita, Osaka, 565-0871, Japan.
L-type amino acid transporter 1 (LAT1, SLC7A5), overexpressed in various cancers, mediates the uptake of essential amino acids crucial for tumor growth. It has emerged as a promising target for cancer therapy. Nanvuranlat (JPH203/KYT-0353), a LAT1 inhibitor, has shown antitumor activity in preclinical studies and efficacy in biliary tract cancer during clinical trials.
View Article and Find Full Text PDFSynthesis, Photophysical Properties and Systematic Evaluation of New Class Fluorescein Based Derivative with Organic Solvents: Spectroscopic and Density Functional Theory Methods for Optoelectronic Applications.
J Fluoresc
January 2025
Department of Physics, Jnanabharathi, Bangalore University, Bengaluru, 560056, Karnataka, India.
In this report the photophysical property of newly synthesized fluorescein based derivative 2-(5-((2,4-dichlorophenyl)diazenyl)-6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid has studied by spectroscopic and theoretical that is by Density Functional Theory technique. The structural and functional group of the synthesized molecule was confirmed by nuclear magnetic resonance and fourier transform infrared spectroscopy technique, and from the result so far obtained has been confirmed that molecule has a stable structure and confirmed the presence the functional groups present in the sample. The optical properties of the molecule are studied using the spectroscopic technique and it has revealed the solute-solvent interaction behaviour of the molecule and it has been observed that the bathochromic shift was of about 5 nm, from the fluorescence measurement it has revealed that the emission has been observed at green region and from the power spectra it has been confirmed the same.
View Article and Find Full Text PDFSynthesis, biological evaluation, and in silico studies of phenyl naphthalene-2-sulfonate derived thiosemicarbazones as potential carbonic anhydrase inhibitors.
Bioorg Chem
February 2025
Institute of Chemical Sciences, Bahauddin Zakariya University, 60800 Multan, Pakistan. Electronic address:
A series of novel phenyl naphthalene-2-sulfonate-based thiosemicarbazones (5a-v) were synthesized and evaluated for their inhibitory activity against human carbonic anhydrases I and II (hCA I and hCA II). Compounds 5d and 5p demonstrated the highest inhibitory potency, with IC values of 4.32 ± 0.
View Article and Find Full Text PDFCinnamic acid conjugated with triazole acetamides as anti-Alzheimer and anti-melanogenesis candidates: an in vitro and in silico study.
Sci Rep
January 2025
Stem Cells Technology Research Center, Shiraz University of Medical Sciences, Shiraz, Iran.
In this study, new cinnamic acid linked to triazole acetamide derivatives was synthesized and evaluated for anti-Alzheimer and anti-melanogenesis activities. The structural elucidation of all analogs was performed using different analytical techniques, including H-NMR, C-NMR, mass spectrometry, and IR spectroscopy. The synthesized compounds were assessed in vitro for their inhibitory activities against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and tyrosinase enzymes.
View Article and Find Full Text PDFThe use of a benign fast-growing cyanobacterial species to control microcystin synthesis from .
Front Microbiol
December 2024
Department of Energy, Environmental and Chemical Engineering, Washington University in St. Louis, St. Louis, MO, United States.
Introduction: (), one of the most prevalent blue-green algae in aquatic environments, produces microcystin by causing harmful algal blooms (HAB). This study investigated the combined effects of nutrients and cyanobacterial subpopulation competition on synthesizing microcystin-LR.
Method: In varied nitrogen and phosphorus concentrations, cyanobacterial coculture, and algicidal DCMU presence, the growth was monitored by optical density analysis or microscopic counting, and the microcystin production was analyzed using high-performance liquid chromatography-UV.
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