Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 17, Issue 11, 2017

Malignant transformation of cells requires specific adaptations of cellular metabolism to support growth and survival. Alterations in cancer central carbon metabolism including aerobic glycolysis, elevated glutaminolysis, dysregulated tricarboxylic acid cycle and pentose phosphate pathway, facilitate cancer development by maintaining viability and building new biomass. Although a variety of oncogenes or tumor suppressors Read More

Multidrug resistance occurs when a tumor develops resistance to multiple chemotherapeutic drugs, which may include antitumor drugs with different chemical structures and mechanisms. Multidrug resistance limits the treatment effects of antitumor drugs, and is the main cause of chemotherapy failure. Multidrug resistance is caused by numerous factors including changes in ATP-binding cassette transporters, targe Read More

Cytokines are small secreted proteins serving as vital mediators that mediate the host immune responses. Transcription and post-transcription play a critical role in cytokine expression through the regulation of message RNA (mRNA) cytoplasmic localization, translation initiation and decay. Researches have been conducted to reveal regulatory mechanisms of cytokines production in cells involved in cancer. AU-rich element ( Read More

Aromatase inhibitors have often been likened to that of 'medical scalpels' for the treatment of breast carcinoma. By inhibiting the singular step of aromatisation, they have proven to be extremely effective allies in the treatment of breast cancer among postmenopausal women. However, their relevance soon may not be limited to the post-menopausal age group alone. Recent studies have hinted at their utility amongst the pre Read More

Background: The epidermal growth factor receptor (EGFR) is a driver oncogene and specific blockade of EGFR has been shown to be an effective therapeutic approach against multiple human cancers. Aims: Here we employed the homogeneous time-resolved fluorescence (HTRF) technology to screen new EGFR mediators. Method: 4 hits (NDS-41107, NDS-41119, NDS-41111 and NDS-41126) were confirmed in a compound libr Read More

Background: Saponins from Medicago species display several biological activities, among them apoptotic effects against plant cells have been evidenced. In contrast, their cytotoxic and antitumor activity against animal cells have not been studied in great details. Objective: To explore the cytotoxic properties of saponin from Medicago species against animal cells and their effect in combination with the antitumoral drug cis Read More

Background: Fruits of Morus alba L. (mulberry) have various bioactive compounds such as polyphenols and anthocyanins and used as a herbal medicine. However, the anti-cancer effects and molecular basis have not been elucidated. Methods: We isolated the cyanidin-3-glucoside in various cultivar of mulberry by acidified-methanol extraction methods. This molecule were compared mass spectroscopic properties by LC-MS/ Read More

Background: Squamous cell cancer is a heterogeneous aggressive disease, therefore, its treatment is challenging. Increased attention has been paid to metal complexes as anticancer drugs. However, new insights towards autophagy have been recognized due to its role in tumor cell death or survival. Objective: To clarify the antitumor activity of copper (I) nicotinate complex (CNC) as new therapeutic agent and understand the Read More

Background: Resveratrol (RV) and its analogues Aza-stilbenes were found effective in exhibiting anticancer activity. Objective: The present study mainly focused on the green synthesis of novel imine stilbene analogues and evaluation of their anticancer activity besides their influence on hypoxia-induced gene expression in cancer cells. Method: Novel imine stilbenes, differing in number and/or position of hydroxyl and met Read More

Background: Renal cell carcinoma (RCC) is one of the most common neoplasms that occurs in the kidney and is marked by a unique biology, with a long history of poor response to conventional cancer treatments. In recent years, there have been significant advancements implemented to understanding the biology of RCC, which has led to the introduction of novel targeted therapies in the management of patients with met Read More

Background: Cabazitaxel (CTX) is a second- generation taxane derivative, a class of potent anticancer drugs with very low water solubility. CTX is used in patients with resistant prostate cancer unresponsive to the first generation taxane, docetaxel. Currently marketed formulations of CTX contain high concentrations of surfactant and ethanol, which cause severe hypersensitivity reactions in patients. Methods: In order to in Read More

Background: Cancer is one of the most dangerous diseases with quite a high mortality rate. Many quinazoline derivatives show potent anticancer activity. Objective: In this work our aim is to develop novel, safe and effective anticancer agents. Method: New 6,8-dibromo-2-(4-chlorophenyl)-quinazoline-sulphonamide hybrids and some Schiff´s base analogs were synthesized, and their structures were confirmed by spectral an Read More

Background: Evidence has been provided of the anti-proliferative activity of citalopram against some cancer cells. Objective: The apoptotic impact of citalopram, an antidepressant, against liver hepatocellular carcinoma cell line HepG2 was investigated in relation to the oxidative pathway and nuclear factor (NF)ΚB activation. Method: The cytotoxic effects of citalopram on HepG2 cells were determined by MTT assay. Reactive o Read More

Background: A new tool for the drug delivery is based on the use of Mesenchymal Stromal Cells (MSCs) loaded in vitro with anti-cancer drugs. Unfortunately, the restricted lifespan of MSCs represents a significant limitation to produce them in high amounts and for long time studies. Immortalized MSCs from adipose tissue (hASCs) have been generated as good source of cells with stable features. These cells could imp Read More

Background: Breast cancer is associated with a high mortality rate around the world due to its aggressiveness and high resistance to conventional therapies. Sanguinarine (SAN) and Chelerythrine (CHE) are plant alkaloids extracted from Sanguinaria canadensis and Macleaya cordata, which have been studied for their bioactivities. Objective: To determine the anticancer activities of Sanguinarine (SAN) and Chelerythrine (CHE) Read More

Background: Human Hsp90 chaperone inhibitors are known to be potential anticancer drugs. Previously we have shown a couple of 5-aryl-4-(2,4-dihydroxyphenyl)-1,2,3-thiadiazoles to be promising anticancer agents. Objective: To improve the compounds containing 4-(2,4-dihydroxyphenyl)-1,2,3-thiadiazole scaffold as human Hsp90 inhibitors. Method: We employed chemical synthesis to obtain new compou Read More

Background: Natural products inhibiting fatty acid synthase are potential therapeutic agents to treat cancer. Objective: To investigate the chemical constituents of the root tubers of Lindera aggregate and the stems of Linderanacusua, and to find natural inhibitors on the expression level on fatty acid synthase in human breast cancer MDA-MB-231 cells. Methods: The isolation and purification of the extracts were conducted by the Read More