Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 17, Issue 6, 2017

Breast cancer has continued to cause high cancer death rates among women worldwide. The use of plants’ natural products in breast cancer treatment has received more attention in recent years due to their potentially wider safety margin and the potential to complement conventional chemotherapeutic drugs. Plantbased products have demonstrated anticancer potential through different biological pathways including Read More

Background: Polymeric micelles can provide a valid way for cancer treatment with several benefits including high water-solubility of lipophilic drugs, low unwanted effects of cytotoxic drugs by way of reduced systemic exposure and prolonged retention time in the circulatory system. Objective: Recently, there is an increasing interest in preparing poly (ethylene glycol)-poly (amino acid) copolymeric micelles as drug delivery carri Read More

Epigenetic modifications play central roles in cellular differentiation and their deregulations really contribute to tumor development. Histone deacetylase (HDAC) enzymes can exert their functions in the epigenetic regulation of gene expression related to oncogenesis via deacetylating the lysine residues of histones in the chromatin and various non-histone proteins. A majority of HDAC inhibitors (HDACIs) have been in differ Read More

Background: Angiogenesis is a fundamental process in the progression, invasion, and metastasis of tumors. Therapeutic drugs such as bevacizumab and ranibuzumab have thus been developed to inhibit vascular endothelial growth factor (VEFG)-promoted angiogenesis. While these anti-angiogenic drugs have been commonly used in the treatment of cancer, patients often develop significant resistance that limits the Read More

Background: Cancer is considered a major public health problem worldwide. Objective: The aim of this paper is to design and synthesis of novel anticancer agents with potent anticancer activity and minimum side effects. Method: A series of pyrrole derivatives were synthesized, their anti-cancer activity against nine cancer cell lines and two non-cancer cell lines were evaluated by MTT assay, and their cell cycle progression Read More

Background: Cancer is a major health problem to human beings around the world. Many quinazoline derivatives were reported to have potent cytotoxic activity. Aims: Our aim in this work is the discovery of potent epidermal growth factor receptor (EGFR) inhibitors with anti-breast cancer activity containing 4-substituted quinazoline pharmacophore. Method: Novel series of 4-substituted 6,8-dibromo-2-(4-chlorophenyl)-quin Read More

Background: Dehydroleucodine, a natural sesquiterpene lactone from Artemisia douglassiana Besser (Argentine) and Gynoxys verrucosa (Ecuador). Objective: To define the molecular mechanisms underlying the effect of dehydroleucodine on the human glioblastoma cells. Method: Various techniques (cDNA expression array, real-time quantitative PCR, chromatin immunprecipitation, luciferase reporter assay, use of phosph Read More

Background: An efficient strategy to improve the immunogenicity of peptide vaccines is the use of a synthetic peptide containing cytotoxic T-lymphocyte (CTL) epitopes with T-helper (Th) inducing-epitopes. Objective: Our purpose was to determine the use of human epidermal growth factor receptor-2 (Her2/neu)- specific CTL epitopes plus the pan HLA DR-binding epitope (PADRE) and CpG oligodeoxynucleotides (ODNs) Read More

Background: The ultimate goal of the study was to find a role of curcumin in targeting lung cancer stem cells by reducing their self-renewal efficiency causing DNA damage. Materials and Methods: Circulating lung cancer stem cells were isolated by sphere formation assay and further analysed by flow-cytometry and qRT-PCR for the presence of stem cell and stem cell transcription markers. The IC50 values of gemcitab Read More

Background: In cancer, apoptosis relevant proteins—such as CaM kinase, Bcl-2 or P53, topoisomerase I, cell migration feature and DNA/BSA—macromolecules represent significant targets for current chemotherapeutics. Objective: We recently reported two coordination compounds—[Cu(C6H16N2O2)2][Ni(CN)4] (1) and [Cu(C6H16 N2O2)Pd(CN)4] (2)—together with their IR spectra, magnetic properties, thermal analys Read More

Background: The high mortality rate of lung cancer is highly associated with faster metastasis spread. All Trans Retinoic Acid (ATRA), being the first choice drug for leukemia therapy is now under intense study for its therapeutic efficiency in other solid cancers. Objectives: This study was aimed to investigate the anti-metastasis activity of free ATRA and liposome entrapped ATRA (5:4:1) in the experimental C57BL/6 mice model deve Read More