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Anticancer activity of Pd complexes 1-5 with bidentate N-heteroaromatic hydrazone ligands was investigated on human acute monocytic leukemia (THP-1; cells in a suspension) and human mammary adenocarcinoma (MCF-7; two-dimensional layer and three-dimensional spheroid tumor model) cell lines. For the Pd(II) complexes with condensation products of ethyl hydrazainoacetate and quinoline-8-carboxaldehyde (complex 1) and 2-formylpyridine (complex 3), for which apoptosis was determined as a mechanism of anticancer activity, further investigation revealed that they arrest the cell cycle in G0/G1 phase, induce generation of reactive oxygen species and inhibit Topoisomerase I in vitro. In silico studies corroborate experimental findings that these complexes show topoisomerase inhibition activity in the micromolar range and indicate binding to a DNA's minor groove as another potential target. Based on the results obtained by circular dichroism and fluorescence spectroscopy measurements, the most active complexes are suitable to be delivered to a blood stream via human serum albumin.
This article was published in the following journal.
Name: Journal of inorganic biochemistry
We synthesized five iron chelator derived from 2,6-diacetylpyridine bis(acylhydrazones) and proved their iron complexes structure by X-ray single crystal diffraction. These ligands have a significant ...
A series of Ln(II) and Ca(II) bis(alkyl) complexes with bulky benzhydryl ligands, [( p- tBu-CH)CH]M(L ) (M = Sm, L = DME, n = 2 (1); M = Sm, Yb, Ca, L = TMEDA, n = 1 (2, 3, 4), were synthesized by the...
Cancer is one of the main causes of death throughout the world. The anticancer agents are indispensable for the treatment of various cancers, but most of them currently on the market are not specific,...
New Pd(II) and Pt(IV) triazine complexes [Pt( )(Cl)(HO)].3Cl.3HO (), [Pt( )(Cl)(HO)].3Cl (), [Pt( )(Cl)(HO)].3Cl (), [Pt( )(Cl)(HO)] .2Cl.4HO (), [Pd( )(HO)] .3Cl (), [Pd( )(HO)].3Cl (), [Pd( )(HO)].3...
This work is focused on the synthesis, characterization, and preliminary biological evaluation of bio-conjugated Au and Cu complexes with the aim of overcoming the well-known side effects of chemother...
The primary objective of this study is to assess the performance of an in silico designed alternative protocol for control of stress hyperglycemia of inpatients treated for Coronary Artery...
The investigators hypothesize that the CXCR2 ligands/CXCR2 biological axis plays an important role in promoting angiogenesis in PC; and that the genetic changes and the microenvironment of...
A Study Evaluating the Safety, Pharmacokinetics, and Anti-tumor Activity of ABBV-321 in Subjects With Advanced Solid Tumors Associated With Overexpression of the Epidermal Growth Factor Receptor (EGFR) or Its Ligands
This is an open-label, Phase 1, dose-escalation study to determine the maximum tolerated dose (MTD) and the recommended phase two dose (RPTD), and to assess the safety, preliminary efficac...
PRECISE is a study to discover new detection, prognosis and treatment biomarkers for cancer. This is a prospective, multi-center, observational study designed to collect de-identified bios...
With this project the investigators aim to investigate whether premature ventricular complexes (PVC) have a prognostic significance in persons without structural heart disease. Further the...
Receptors of CLONIDINE and other IMIDAZOLINES. Activity of the ligands was earlier attributed to ADRENERGIC ALPHA-2 RECEPTORS. Endogenous ligands include AGMATINE, imidazoleacetic acid ribotide, and harman.
A proton ionophore. It is commonly used as an uncoupling agent and inhibitor of photosynthesis because of its effects on mitochondrial and chloroplast membranes.
Complexes containing CHLOROPHYLL and other photosensitive molecules. They serve to capture energy in the form of PHOTONS are generally found as components of the PHOTOSYSTEM I PROTEIN COMPLEX or the PHOTOSYSTEM II PROTEIN COMPLEX.
Neutral or negatively charged ligands bonded to metal cations or neutral atoms. The number of ligand atoms to which the metal center is directly bonded is the metal cation's coordination number, and this number is always greater than the regular valence or oxidation number of the metal. A coordination complex can be negative, neutral, or positively charged.
Complexes of iodine and non-ionic SURFACE-ACTIVE AGENTS acting as carrier and solubilizing agent for the iodine in water. Iodophors usually enhance bactericidal activity of iodine, reduce vapor pressure and odor, minimize staining, and allow wide dilution with water. (From Merck Index, 11th ed)
Leukemia is a type of cancer of the blood or bone marrow characterized by an abnormal increase of immature white blood cells called "blasts". Leukemia is a broad term covering a spectrum of diseases. In turn, it is part of the even broader grou...