Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 20, Issue 3, 2020

Background: Cancer is increasingly becoming the leading cause of death in many countries, and malignant tumours of the digestive system account for majority of cancer incidence and mortality cases. Metabolism has been identified as a core hallmark of cancer. Peroxisome proliferator activated receptor gamma coactivator-1 alpha (PGC-1α) is a pivotal regulator of mitochondrial energy metabolism. Accumulating eviden Read More

Background: Conjugation of triterpenoids such as betulinic acid 1 with the Triphenylphosphonium (TPP) group is a powerful approach to generating medicinal compounds. Their development proposes structure optimization in respect of availability and activity towards target cells and organelles. Selection of 1 or its precursor betulonic acid 2 and the optimal linker is of particular importance for drug candidate identification among Read More

Background and Objective: Drug resistance and adverse effects are immense healthcare challenges in cancer therapy. Benzimidazole ring-based small molecules have been effective anticancer agents in drug development. In an effort to develop novel chemotherapeutics, we synthesized and assessed the anticancer and antibacterial activities of a small library of structurally unique benzimidazoles. Methods: The benzimidazole Read More

Background and Objective: Prostate cancer is the second cause of death in men worldwide. In this study, the cytotoxic effects of PLGA polymer-coated gold Magnetic Nanoparticles (MGNPs), as a novel treatment to enhance radiation and thermal sensitivity in the presence of hyperthermia (43°C) and electron beam, on DU145 prostate cancer cells were investigated. Methods: Nanoparticles were characterized using TEM, DL Read More

Background: Chronic Lymphocytic Leukaemia (CLL) is an indolent disorder, which mainly affects older adults. Since the advent of chemoimmunotherapy, great progress has been made in its treatment. However, some patients develop a more aggressive form of the disease and are included in the group of high-risk CLL patients with a dismal prognosis and a need for new therapies. Objective: Maltotriose-mod Read More

Background: Thiophene, thiazole, and isoxazole derivatives are present in a wide range of natural and synthetic compounds with heterogeneous pharmacological activity. Due to their structural diversity, they are some of the most versatile classes of compounds for anticancer drug design and discovery. Objective: Thiophene, thiazole, and isoxazole derivatives were herein designed with a dual purpose: as antiproliferative agent Read More

Background: The first choice of treatment in Hepatocellular Carcinoma (HCC) is 5-fluorouracil (5-FU). Nitroxoline (NIT), a potent inhibitor of Cathepsin B, impairs tumor progression by decreased extracellular matrix degradation. The objective of the current project was designed to target nanoparticles for co-delivery of 5-FU and NIT in order to enhance the 5-FU cytotoxic effects and reduce the metastatic properties of Hep Read More

Background: Hybrid molecules combining uracil skeleton with methylidene exo-cyclic group were designed in the search for novel anticancer drug candidates. Objective: Two series of racemic 5-methylidenedihydrouracils, either 1,3-disubstituted or 1,3,6-trisubstituted were synthesized and tested for their possible cytotoxic activity against two cancer cell lines (HL-60 and MCF-7) and two healthy cell lines (HUVEC and MCF-10 Read More

Background: Heat shock protein 90 (Hsp90) is an encouraging anticancer target for the development of clinically significant molecules. Schiff bases play a crucial role in anticancer research because of their ease of synthesis and excellent antiproliferative effect against multiple cancer cell lines. Therefore, we started our research work with the discovery of resorcinol/4-chloro resorcinol derived Schiff bases as Hsp90 inhibitors, wh Read More

Background: To block the metastatic and angiogenic pathways during the tumor progression arouses considerable pharmacological interests in the development of anticancer drugs. Objective: To develop alternative antiangiogenic and antimetastic agents, we designed and prepared a series of nature inspired isomalyngamide A analogs containing ribose conjugate with 1,2-diaminoethane or 1,3- diaminopropane linkers (1-8). Met Read More