Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 20, Issue 7, 2020

Breast cancer has been identified as one of the main cancer-related deaths among women during some last decades. Recent advances in the introduction of novel potent anti-cancer therapeutics in association with early detection methods led to a decrease in the mortality rate of breast cancer. However, the scenario of breast cancer is yet going on and further improvements in the current anti-cancer therapeutic approa Read More

Background: Angiogenesis marks key progress in the growth, recurrence, and metastasis of various cancers. Antiangiogenic drugs can improve the blood supply and oxygen content of tumors and enhance the effects of chemotherapy and radiotherapy by normalizing tumor blood vessels and microenvironment. The further recent developments of Immune Checkpoint Inhibitors (ICIs) provide significant progress in cancer immu Read More

Limitations on the pharmacotherapy and a high prevalence worldwide are critical issues related to depression and cancer. It has been discussed that a dysregulation of intracellular Ca2+ homeostasis is involved in the pathogenesis of both these diseases. In addition, depression raises the risk of cancer incidence. Consistent data support the concept that depression is an independent risk issue for cancer. However, the cellular Read More

Background: Targeting Cancer Stem-Like Cells (CSLCs) can provide promising new therapeutic strategies to inhibit cancer progression, metastasis and recurrence. Salinomycin (Sal), an antibacterial ionophore, has been shown to inhibit CSCs specifically. Recently, it has been reported that Sal can destabilize TAZ, the hypo pathway transducer in CSLCs. Objectives: Here, in the current study, we aimed to assess the differential to Read More

Background and Purpose: Melittin, as the main ingredient of honeybee venom, that has shown anticancer properties. The present study aimed at investigating the cytotoxic impacts of melittin on 4T1 breast cancer cells. Methods: Hemolytic activity of different concentrations (0.125, 0.25, 0.5, 1, 2, 4, 8μg/ml) of melittin was assayed and then cytotoxicity of selected concentrations of melittin (2, 4, 8, 16, 32, and 64μg/ml), 2 and Read More

Background: MicroRNAs (miRs) are a group of small non-coding and single-stranded RNAs of 18 to 25 nucleotides. The study of microRNAs is one of the new ways to detect cancer. In this study, the serum expression of miR-223 in patients with GC was measured and compared with the control group. Methods: This case-control study was conducted on 39 patients with GC and 39 control subjects who visited the Reza Radiotherap Read More

Background and Objective: The present study was carried out to evaluate the anticancer property of an alkylamino phenol derivative -2-((3,4-Dihydroquinolin-1(2H)-yl)(p-tolyl)methyl)phenol) (THTMP) against human breast cancer cells. The cytotoxicity of the THTMP was assessed to know its specificity towards breast cancer cells without affecting the normal cells. Methods: The THTMP was synthesized and the cytotoxicity w Read More

Background: Nucleotide-binding domain Leucine-rich Repeat Protein 3 (NLRP3) plays a regulatory role in the immune and inflammatory responses, and has been implicated in Colorectal Cancer (CRC) progression and metastasis. However, the underlying molecular mechanisms have not been fully elucidated. Methods: In this study, we analyzed the expression levels of NLRP3 in human CRC tissues, and performed functional ass Read More

Background: Phosphoinositide-Dependent Kinase 1 (PDK1) is now widely studied in malignant solid tumors. Researchers have previously revealed that targeting PDK1 is thought of as a promising anticancer treatment strategy. The aim of this study was designed to evaluate the anticancer activity of GSK-470, a novel and highly specific inhibitor of PDK1, in Pheochromocytoma (PCC) tumor model. Methods: PC12 cells were x Read More

Background: microRNAs are known to regulate various protein-coding gene expression posttranscriptionally. Fatty acids are cell membrane constituents and are also known to influence the biological activities of the cells like signal transduction, growth and differentiation of the cells, apoptosis induction, and other physiological functions. In our experiments, we used lauric acid to analyse its effects on human cancerou Read More

Background: Accounting for mortality nearly one in four of human and second highest leading cause of death worldwide. Every year, about 10 million new cancers are diagnosed and causing major health issues in both developing and developed countries. Methods: A series of new dihydrazones were synthesized and screened for in vitro anticancer activity against three different MDA-MB-231, A546 and MCF7 cell lin Read More

Background and Objective: Cancer incidence is 24% higher in children and young adults exposed to Computed Tomography (CT) scans than those unexposed. Non-repairing of ionizing radiation-induced DNA Double-Strand Breaks (DSBs) can initiate carcinogenesis. In the present study, we aimed to investigate the radioprotective potential of melatonin against DSBs in peripheral blood lymphocytes of patients undergoing abd Read More

Background: Hepatocellular Carcinoma (HCC), the second leading cause of cancer-related mortality with over half a million new cases diagnosed annually in the world, accounts for nearly 70% of cancer deaths in parts of Asia and Africa. Podophyllum, one of the important members of the lignane class of natural products derived from plants in Podophyllum peltatum L., has been shown to suppress tumor growth in various c Read More

Background: Breast Cancer Stem Cells (BCSCs) possess the ability of self-renewal and cellular heterogeneity, and therefore, play a key role in the initiation, propagation and clinical outcome of breast cancer. It has been shown that ferrocene complexes have remarkable potential as anticancer drugs. Objective: The present study was conducted to investigate the effects of a novel ferrocene complex, 1- ferrocenyl-3-(4-methylsulf Read More

Background: Currently, most of the drugs used in clinical applications show their pharmacological influences by inhibiting or activating enzymes. Therefore, enzyme inhibitors have an essential place in the drug design for many diseases. Objective: The current study aimed to contribute to this growing drug design field (i.e., medicine discovery and development) by analyzing enzyme-drug interactions. Methods: For this reason, P Read More

Indroduction: This article presents a theoretical analysis of the safe form and dosage of the amygdalin derivative. By making a precise socio-anthropological analysis of the life of the ancient people of Botra (Hunza people, Burusho/Brusho people), a hypothesis has been postulated through a number of modern quantum-mechanical, molecular-topological and bio analytical checks, and has also been confirmed by tw Read More

Background: The derivatives of xanthene are known to have promising anticancer properties, in comparison to xanthene itself. Objective: The object of our study was to develop few xanthene derivatives (a family of fifteen novel 3,4,6,7- tetrahydro-3,3-dimethyl-9-phenyl-2H-xanthene-1,8(5H, 9H)-diones encoded as 4a-4m), which were effectively prepared through regioselective synthesis approach, and to test their anti Read More