Design, Synthesis, and Characterization of Novel Thiazolidine-2,4-Dione-Acridine Hybrids as Antitumor Agents.

This study focuses on the synthesis and structural characterization of new compounds that integrate thiazolidine-2,4-dione, acridine moiety, and an acetamide linker, aiming to leverage the synergistic effects of these pharmacophores for enhanced therapeutic potential. The newly designed molecules were efficiently synthesized through a multi-step process and subsequently transformed into their hydrochloride salts. Comprehensive spectroscopic techniques, including nuclear magnetic resonance (NMR), high-resolution mass spectrometry (HRMS), infrared (IR) spectroscopy, and elemental analysis, were employed to determine the molecular structures of the synthesized compounds.

Design, Synthesis, and Evaluation of Novel Indole Hybrid Chalcones and Their Antiproliferative and Antioxidant Activity.

The synthesis, anticancer, and antioxidant activities of a series of indole-derived hybrid chalcones are reported here. First, using the well-known Claisen-Schmidt condensation method, a set of 29 chalcones has been designed, synthesized, and consequently characterized. Subsequently, screening for the antiproliferative activity of the synthesized hybrid chalcones was performed on five cancer cell lines (HCT116, HeLa, Jurkat, MDA-MB-231, and MCF7) and two non-cancer cell lines (MCF-10A and Bj-5ta).

Chalcone-Acridine Hybrid Suppresses Melanoma Cell Progression via G2/M Cell Cycle Arrest, DNA Damage, Apoptosis, and Modulation of MAP Kinases Activity.

This study was focused on investigating the antiproliferative effects of chalcone hybrids in melanoma cancer cells. Among seven chalcone hybrids, the chalcone-acridine hybrid was the most potent and was selected for further antiproliferative mechanism studies. This in vitro study revealed the potent antiproliferative effect of via cell cycle arrest and apoptosis induction.

Programmed Cell Death Alterations Mediated by Synthetic Indole Chalcone Resulted in Cell Cycle Arrest, DNA Damage, Apoptosis and Signaling Pathway Modulations in Breast Cancer Model.

Although new chemotherapy significantly increased the survival of breast cancer (BC) patients, the use of these drugs is often associated with serious toxicity. The discovery of novel anticancer agents for BC therapy is expected. This study was conducted to explore the antiproliferative effect of newly synthesized indole chalcone derivative ZK-CH-11d on human BC cell lines.

Design and synthesis of novel tacrine-indole hybrids as potential multitarget-directed ligands for the treatment of Alzheimer's disease.

The authors report on the synthesis and biological evaluation of new compounds whose structure combines tacrine and indole moieties. Tacrine-indole heterodimers were designed to inhibit cholinesterases and β-amyloid formation, and to cross the blood-brain barrier. The most potent new acetylcholinesterase inhibitors were compounds and (IC = 25 and 39 nM, respectively).

The Newly Synthetized Chalcone L1 Is Involved in the Cell Growth Inhibition, Induction of Apoptosis and Suppression of Epithelial-to-Mesenchymal Transition of HeLa Cells.

Over the past decades, natural products have emerged as promising agents with multiple biological activities. Many studies suggest the antioxidant, antiangiogenic, antiproliferative and anticancer effects of chalcones and their derivatives. Based on these findings, we decided to evaluate the effects of the newly synthetized chalcone L1 in a human cervical carcinoma cell (HeLa) model.

Mechanochemical Synthesis and Isomerization of -Substituted Indole-3-carboxaldehyde Oximes †.

Performing solution-phase oximation reactions with hydroxylamine hydrochloride (NHOH·HCl) carries significant risk, especially in aqueous solutions. In the present study, four -substituted indole-3-carboxaldehyde oximes were prepared from the corresponding aldehydes by solvent-free reaction with NHOH·HCl and a base (NaOH or NaCO) using a mechanochemical approach, thus minimizing the possible risk. In all cases, the conversion to oximes was almost complete.

Liquid chromatographic chiral recognition of phytoalexins on immobilized polysaccharides chiral stationary phases. Unusual temperature behavior.

Three immobilized polysaccharide chiral stationary phases, Chiralpak IA, Chiralpak IB and Chiralpak IC, were used for the study of enantioseparation of 36 derivatives of natural indole phytoalexins, in most cases bioactive, including racemic spirobrassinin, 1-methoxyspirobrassinin and 1-methoxyspirobrassinol methyl ether. Almost all analytes were baseline resolved at least on two different polysaccharide columns in normal phase mode. The effects of mobile phase composition, the analyte structure and the column temperature on the retention and enantioseparation were investigated.

New chalcone derivative exhibits antiproliferative potential by inducing G2/M cell cycle arrest, mitochondrial-mediated apoptosis and modulation of MAPK signalling pathway.

In the present study, we investigated antiproliferative activity of seven newly synthesized chalcone derivatives. Among tested compounds, (2 E)-3-(acridin-9-yl)-1-(2,6-dimethoxyphenyl)prop-2-en-1-one (1C) was the most potent with IC = 4.1 μmol/L in human colorectal HCT116 cells and was selected for further studies.

[Computer tomography in the diagnosis of neuromuscular diseases in children].

Recently in the literature occasional reports were published on the use of computed tomography (CT) in the diagnosis of neuromuscular diseases. The authors compared in a group of 23 children aged 3 to 15 years the results of clinical, laboratory, electromyographic, bioptic and CT findings on muscles. Only in four children the result of CT did not correlate with the clinical finding because of the incipient stage of the disease with structural changes which were yet only slightly expressed.

[The importance of the gammagraphic examination of the skeleton in the diagnostic and therapeutic strategy in carcinoma of the prostate].

One hundred and sixty patients with the diagnosis of prostate cancer have been treated at the Research Institute of Clinical and Experimental Oncology in Brno over the last 10 years. The present paper has been devoted to the diagnostics of skeleton by scintigraphy as compared with X-ray examination of bones. Scintiscanning of skeleton was performed on a gamma-graph Picker 500 i, 99mTc pyrophosphate was used and scintiscanning was performed in the usual examination regimen.

Cytologic grading in relation to the clinical stage of the breast cancer.

Cytologic grading which may be performed at the same time as diagnostic cytology seems to be of a value in the pathobiology of the breast cancer. Other methods, such as mammography, termography, xenography, histological grading and some biological markers help to establish biological behavior of the tumor and appropriate treatment approach. In spite of the progress in diagnosis and therapy many problems remain to be clarified.

Study of radiation dose fractionation in some tumor types.

In the presented work we have tested another fractionation schemes than simple fractionation in some so-called radioresistant tumors, i. e. in breast cancer and malignant melanoma.