scholarly journals Avobenzone incorporation in a diverse range of Ru(ii) scaffolds produces potent potential antineoplastic agents

2020 ◽  
Vol 49 (35) ◽  
pp. 12161-12167
Author(s):  
Raphael T. Ryan ◽  
Dmytro Havrylyuk ◽  
Kimberly C. Stevens ◽  
L. Henry Moore ◽  
Doo Young Kim ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Antineoplastic Agents ◽  
Ruthenium Complexes ◽  
Diverse Range ◽  
Parent Ligand

Four structurally distinct classes of polypyridyl ruthenium complexes containing avobenzone exhibited low micromolar and submicromolar potencies in cancer cells, and were up to 273-fold more active than the parent ligand.

Light activation of cyclometalated ruthenium complexes drives towards caspase 3 dependent apoptosis in gastric cancer cells

2020 ◽  
Vol 208 ◽  
pp. 111080 ◽  
Author(s):  
Jorge Andrés Solís-Ruiz ◽  
Anaïs Barthe ◽  
Gilles Riegel ◽  
Rafael Omar Saavedra-Díaz ◽  
Christian Gaiddon ◽  
...  
Keyword(s):  
Gastric Cancer ◽  
Cancer Cells ◽  
Caspase 3 ◽  
Ruthenium Complexes ◽  
Light Activation ◽  
Gastric Cancer Cells

How Antimalarials and Antineoplastic Drugs can Interact in Combination Therapies: a Perspective on the Role of PPT1 Enzyme

2021 ◽  
Vol 22 ◽  
Author(s):  
Diana Duarte ◽  
Nuno Vale
Keyword(s):  
Cancer Cells ◽  
Cancer Progression ◽  
Antineoplastic Agents ◽  
Antimalarial Drugs ◽  
Antineoplastic Drugs ◽  
Anticancer Effects ◽  
Different Types ◽  
Important Pathway ◽  
Palmitoyl Protein Thioesterase

: Antimalarial drugs from different classes have demonstrated anticancer effects in different types of cancer cells, but their complete mode of action in cancer remains unknown. Recently, several studies reported the important role of palmitoyl-protein thioesterase 1 (PPT1), a lysosomal enzyme, as the molecular target of chloroquine and its derivates in cancer. It was also found that PPT1 is overexpressed in different types of cancer, such as breast, colon, etc. Our group has found a synergistic interaction between antimalarial drugs, such as mefloquine, artesunate and chloroquine and antineoplastic drugs in breast cancer cells, but the mechanism of action was not determined. Here, we describe the importance of autophagy and lysosomal inhibitors in tumorigenesis and hypothesize that other antimalarial agents besides chloroquine could also interact with PPT1 and inhibit the mechanistic target of rapamycin (mTOR) signalling, an important pathway in cancer progression. We believe that PPT1 inhibition results in changes in the lysosomal metabolism that result in less accumulation of antineoplastic drugs in lysosomes, which increases the bioavailability of the antineoplastic agents. Taken together, these mechanisms help to explain the synergism of antimalarial and antineoplastic agents in cancer cells.

Construction of indazolo[3,2-a]isoquinolines via [3 + 2] cycloaddition of benzynes

2019 ◽  
Vol 17 (40) ◽  
pp. 8963-8968 ◽  
Author(s):  
Yue-Kun Li ◽  
Ming-Xin Cui ◽  
Feng Sha ◽  
Qiong Li ◽  
Xin-Yan Wu
Keyword(s):  
Cancer Cells ◽  
Proliferative Activity ◽  
Diverse Range ◽  
Azomethine Imines

A [3 + 2] annulation protocol for the construction of N-substituted indazolo[3,2-a]isoquinolines starting from benzynes and C,N-cyclic azomethine imines was developed. A diverse range of indazolo[3,2-a]isoquinolines can be easily accessed, which show good anti-proliferative activity on cancer cells.

scholarly journals Use of a Zebrafish Model to Evaluate Toxicity of Schiff Base Complexes of Copper (II) and Zinc (II) as Possible Antineoplastic Agents

Proceedings ◽  
2019 ◽  
Vol 22 (1) ◽  
pp. 11
Author(s):  
Claudia Cardozo ◽  
Andreas Reiber ◽  
Veronica Akle
Keyword(s):  
Schiff Base ◽  
Cancer Cells ◽  
Antineoplastic Agents ◽  
Promising Result ◽  
Organometallic Complexes ◽  
Schiff Base Complexes ◽  
World Health ◽  
Proliferating Cells ◽  
Zebrafish Model ◽  
Toxic Activity

Cancer continues to be one of the leading causes of death, according to the World Health Organization, and chemotherapy is its principal treatment. Organometallic complexes with copper (II) and zinc (II) with Schiff bases as ligand, capable of interacting with cancer cells’ DNA under physiological conditions, may work as good chemotherapy agents because they are less toxic to healthy cells than to cancerous ones. In view of the above, this work focuses on obtaining new Schiff base ligands and their copper and zinc complexes and characterizing them by nuclear magnetic resonance, mass spectrometry, infrared spectroscopy, and other spectroscopic and spectrometric techniques. The objective is to evaluate the toxic activity of the new molecules using the fast proliferating cells of the zebrafish model during development. The toxicity test was performed in zebrafish embryos at 8, 24, 48 and 72 h post fertilization, and a survival and malformation index were registered. Preliminary results show a dose-related effect of the designed Schiff ligands and complexes on the toxicity of the zebrafish embryo and larvae. The survival and malformation index are more severe when exposure occurs during early developmental stages, when cell division is higher due to rapid organization and growth of the new organism. This is a promising result, as the molecules might be cytotoxic to highly proliferating cells, as it occurs in cancer cells. This work represents one of the very few examples that use the zebrafish model to evaluate the cytotoxic activity of Schiff base complexes. Developing the animal model to test the effect of Schiff ligands and their complexes is an important first step to assess the effectiveness of new molecules as antineoplastic agents.

New Cell Cycle Inhibitors Target Aneuploidy in Cancer Therapy

2019 ◽  
Vol 59 (1) ◽  
pp. 361-377 ◽  
Author(s):  
Masanori Kawakami ◽  
Xi Liu ◽  
Ethan Dmitrovsky
Keyword(s):  
Cancer Cells ◽  
Chromosome Segregation ◽  
Antineoplastic Agents ◽  
Spindle Assembly Checkpoint ◽  
Critical Level ◽  
New Agents ◽  
Chromosome Missegregation ◽  
Diploid Cells ◽  
Cell Cycle Inhibitors ◽  
Proliferative Advantage

Aneuploidy is a hallmark of cancer. Defects in chromosome segregation result in aneuploidy. Multiple pathways are engaged in this process, including errors in kinetochore-microtubule attachments, supernumerary centrosomes, spindle assembly checkpoint (SAC) defects, and chromosome cohesion defects. Although aneuploidy provides an adaptation and proliferative advantage in affected cells, excessive aneuploidy beyond a critical level can be lethal to cancer cells. Given this, enhanced chromosome missegregation is hypothesized to limit survival of aneuploid cancer cells, especially when compared to diploid cells. Based on this concept, proteins and pathways engaged in chromosome segregation are being exploited as candidate therapeutic targets for aneuploid cancers. Agents that induce chromosome missegregation and aneuploidy now exist, including SAC inhibitors, those that alter centrosome fidelity and others that are under active study in preclinical and clinical contexts. This review explores the therapeutic potentials of such new agents, including the benefits of combining them with other antineoplastic agents.

scholarly journals Cytotoxicity and anti-tumor effects of new ruthenium complexes on triple negative breast cancer cells

PLoS ONE ◽  
2017 ◽  
Vol 12 (9) ◽  
pp. e0183275 ◽  
Author(s):  
Cecília P. Popolin ◽  
João P. B. Reis ◽  
Amanda B. Becceneri ◽  
Angélica E. Graminha ◽  
Márcio A. P. Almeida ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Triple Negative Breast Cancer ◽  
Breast Cancer Cells ◽  
Triple Negative ◽  
Ruthenium Complexes

scholarly journals Targeting of the mitochondrion by dinuclear thiolato-bridged arene ruthenium complexes in cancer cells and in the apicomplexan parasite Neospora caninum

Metallomics ◽  
2019 ◽  
Vol 11 (2) ◽  
pp. 462-474 ◽  
Author(s):  
Afonso P. Basto ◽  
Nicoleta Anghel ◽  
Riccardo Rubbiani ◽  
Joachim Müller ◽  
David Stibal ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Neospora Caninum ◽  
Ruthenium Complexes ◽  
Apicomplexan Parasite ◽  
Dinuclear Ruthenium ◽  
Dinuclear Ruthenium Complexes

Dinuclear ruthenium complexes inhibit N. caninum and specifically target the parasite mitochondria.

Synthesis and biological properties of tetranuclear ruthenium complexes containing the bis[4(4′-methyl-2,2′-bipyridyl)]-1,7-heptane ligand

2019 ◽  
Vol 48 (38) ◽  
pp. 14505-14515 ◽  
Author(s):  
Biyun Sun ◽  
Madhu K. Sundaraneedi ◽  
Hannah M. Southam ◽  
Robert K. Poole ◽  
Ian F. Musgrave ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Cancer Cells ◽  
Anticancer Agent ◽  
Ruthenium Complexes ◽  
Biological Properties ◽  
Highly Active ◽  
Non Linear

The non-linear polypyridylruthenium(ii) complex (Rubb7-TNL) exhibited good antimicrobial activity, but surprisingly was also highly active against cancer cells. The results suggest Rubb7-TNL may have potential as a new anticancer agent.

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