Anti-Cancer Agents in Medicinal Chemistry
New Issue :: Anti-Cancer Agents in Medicinal Chemistry 17, Issue 3
Anti-Cancer Agents in Medicinal Chemistry aims to cover all the latest and outstanding developments in medicinal chemistry and rational drug design for the discovery of anti-cancer agents.
Each issue contains a series of timely in-depth reviews and guest edited issues written by leaders in the field covering a range of current topics in cancer medicinal chemistry. The journal only considers high quality research papers for publication.
Anti-Cancer Agents in Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments in cancer drug discovery.
Articles from the journal Anti-Cancer Agents in Medicinal Chemistry 17, Issue 3:
- EDITORIAL: Radiopharmaceuticals for Cancer Therapy and Diagnosis
- Targeted Therapy Towards Cancer-A Perspective
- Radiopharmaceuticals in Tumor Hypoxia Imaging: A Review Focused on Medicinal Chemistry Aspects
- Radiolabeled Nanoparticles for Cancer Diagnosis and Therapy
- Nano-Hydroxyapatite Doped with Ho-166 as Drug Delivery System for Bone Cancer Therapy and Diagnosis: Developing a Theragnostic Radiopharmaceuticals
- Hepato and Cardiotoxicity of Chemotherapeutic Treatment Evaluated by Means of Small Animal Imaging
- Plant Derived Inhibitor Sulforaphane in Combinatorial Therapy Against Therapeutically Challenging Pancreatic Cancer
- Natural Compounds A Weapon to Ameliorate Breast Cancer Cells: A Review
- Glucose Oncometabolism of Esophageal Cancer
- Design and Synthesis of Coumarin Derivatives as Novel PI3K Inhibitors
- Effects of Epirubicin and Cisplatin Against 4T1 Breast Cancer Cells are Enhanced by Myrtucommulone-A
- Coumarin Derivatives as Anti-inflammatory and Anticancer Agents
- Copper(II) Complexes with Saccharinate and Glutamine as Antitumor Agents: Cytoand Genotoxicity in Human Osteosarcoma Cells
- New Poly(3-hydroxybutyrate) Microparticles with Paclitaxel Sustained Release for Intraperitoneal Administration
- A Facile and Microwave-assisted Rapid Synthesis of 2-Arylamino-4-(3′-indolyl)- thiazoles as Apoptosis Inducing Cytotoxic Agents
- Fe3O4 Nanoparticles Mediated Synthesis of Novel Isatin-dihydropyrimidinone Hybrid Molecules as Antioxidant and Cytotoxic Agents
- Synthesis, Molecular Docking Study and in vitro Anticancer Activity of Tetrazole Linked Benzochromene Derivatives
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Editor’s Choice – “Differential Cytotoxicity, Cellular Uptake, Apoptosis and Inhibition of BRCA1 Expression of BRCA1-Defective and Sporadic Breast Cancer Cells Induced by an Anticancer Ruthenium(II)-Arene Compound, RAPTA-EA1″
Journal: Anti-Cancer Agents in Medicinal Chemistry
Author(s): Adisorn Ratanaphan, Tidarat Nhukeaw, Khwanjira Hongthong and Paul J Dyson
Abstract
Background: The RAPTA-EA1 complex [ruthenium(II)-arene 1,3,5-triaza-7-phosphaadamantane (pta) complex with an arene-tethered ethacrynic acid ligand] has been reported to overcome drug resistance that developed due to the current use of platinum-based treatments. However, the exact mechanism of action of RAPTA-EA1 remains largely unexplored and unknown.
Objective: Here we have further studied the effect of RAPTA-EA1 on BRCA1-defective HCC1937 breast cancer cells and compared its effects on BRCA1-competent MCF-7 breast cancer cells.
Method: HCC1937 and MCF-7 breast cancer cells were treated with the RAPTA-EA1 complex. The cytotoxicity of ruthenium-induced cells was evaluated by a MTT assay. Cellular uptake of ruthenium was determined by ICP-MS. Cell cycle and apoptosis were assessed using a flow cytometer. Expression of BRCA1 mRNA and its encoded protein was quantitated by a real-time RT-PCR and Western blotting.
Results: Differences in cytotoxicity were correlated with the differential accumulations of ruthenium and the induction of apoptosis. The ruthenium complex caused dramatically more damage to the BRCA1 gene in the BRCA1-defective HCC1937 cells than to the BRCA1-competent MCF-7 cells. It decreased the expression of BRCA1 mRNA in the BRCA1-competent cells, while in contrast, its expression increased in the BRCA1-defective cells. However, the expression of the BRCA1 protein was significantly reduced in both types of breast cancer cells.
Conclusion: The results presented here have demonstrated a differential cellular response for the BRCA1-defective and BRCA1-competent breast cancer cells to RAPTA-EA1. These findings have provided more insight into the actions and development of the ruthenium-based compounds for use for the treatment of breast cancer.
Read more here: http://benthamscience.com/journals/anti-cancer-agents-in-medicinal-chemistry/volume/17/issue/2/page/212/
