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Design, synthesis, and anticancer evaluation of N4-substituted thiosemicarbazones derived from ortho- and para-ethoxy-benzaldehydes.
Spectrochim Acta A Mol Biomol Spectrosc
December 2024
Department of Chemistry, National Institute of Technology-Tiruchirappalli, Tamil Nadu 620015, India. Electronic address:
R - C(S) - NH - N = CH - R [R = o-OCHCH & R = CHN (2-EBP), R = o-OCHCH & R = CHNO (2-EBM), R = p-OCHCH & R = CHN (4-EBP), and R = p-OCHCH & R = CHNO (4-EBM)] have been synthesized. The ligands have been verified via various spectroscopic methods such as IR, NMR, etc. Single-crystal X-ray diffraction methods were applied to identify the structure of 4-EBP.
View Article and Find Full Text PDFDeveloping a Palladium(II) Agent to Overcome Multidrug Resistance and Metastasis of Liver Tumor by Targeted Multiacting on Tumor Cell, Inactivating Cancer-Associated Fibroblast and Activating Immune Response.
J Med Chem
September 2024
State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources/Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources (Ministry of Education of China), Collaborative Innovation Center for Guangxi Ethnic Medicine, School of Chemistry and Pharmaceutical Sciences, Guangxi Normal University, Guilin, Guangxi 541004, PR China.
To targeted overcome the multidrug resistance (MDR) and metastasis of liver tumors, we proposed to develop a palladium (Pd) agent based on a specific residue of human serum albumin (HSA) for multiacting on tumor cell and other components in the tumor microenvironment. To this end, a series of Pd(II) 2-acetylpyridine thiosemicarbazone compounds were optimized to obtain a Pd(II) compound (5b) with significant cytotoxicity against HepG2/ADM cells. Subsequently, we constructed a HSA-5b complex delivery system and revealed the structural mechanism of HSA delivering 5b.
View Article and Find Full Text PDFGeneration of human hepatobiliary organoids with a functional bile duct from chemically induced liver progenitor cells.
Stem Cell Res Ther
August 2024
Department of Surgery, Nagasaki University Graduate School of Biomedical Sciences, 1-7-1 Sakamoto, Nagasaki, 852-8102, Japan.
Background: Liver disease imposes a significant medical burden that persists due to a shortage of liver donors and an incomplete understanding of liver disease progression. Hepatobiliary organoids (HBOs) could provide an in vitro mini-organ model to increase the understanding of the liver and may benefit the development of regenerative medicine.
Methods: In this study, we aimed to establish HBOs with bile duct (BD) structures and mature hepatocytes (MHs) using human chemically induced liver progenitor cells (hCLiPs).
Preliminary evaluation of the toxicological, antioxidant and antitumor activities promoted by the compounds 2,4-dihydroxy-benzylidene-thiosemicarbazones an in silico, in vitro and in vivo study.
An Acad Bras Cienc
May 2024
Federal of Pernambuco, Department of Antibiotics, Laboratory of Chemistry and Therapeutic Innovation, Avenida Professor Moraes Rego, s/n, Iputinga, 50670-901 Recife, PE, Brazil.
Thiosemicarbazones are promising classes of compounds with antitumor activity. For this study, six 2,4-dihydroxy-benzylidene-thiosemicarbazones compounds were synthesized. These compounds were submitted to different assays in silico, in vitro and in vivo to evaluate the toxicological, antioxidant and antitumor effects.
View Article and Find Full Text PDFThiosemicarbazone Mixed-Valence Cu(I/II) Complex against Lung Adenocarcinoma Cells through Multiple Pathways Involving Cuproptosis.
J Med Chem
June 2024
Laboratory of Respiratory Diseases, The Affiliated Hospital of Guilin Medical University, Guilin 541001, P. R. China.
Induction of cuproptosis and targeting of multiple signaling pathways show promising applications in tumor therapy. In this study, we synthesized two thiosemicarbazone-copper complexes ([Cu(L)Cl] 1 and [CuCu(L)Cl] 2, where HL is the ()--methyl-2-(phenyl(pyridin-2-yl)methylene ligand), to assess their antilung cancer activities. Both copper complexes showed better anticancer activity than cisplatin and exhibited hemolysis comparable to that of cisplatin.
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