Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 22, Issue 17, 2022

Currently, chemotherapy is still the main strategy for cancer treatment. However, chemotherapy resistance remains a challenge. Disulfiram (DSF) is an FDA-approved medicine for the treatment of alcoholism; however, it was later revealed to have anticancer properties. Importantly, numerous studies have shown that DSF can be employed as a chemotherapeutic sensitizer to enhance the anticancer efficacy of chemo-drugs in a Read More

Gastric cancer (GC) is the fifth most common type of tumor and the third leading cause of cancer death worldwide. The evolution of gastric carcinogenesis is still poorly understood and, for this reason, preclinical research protocols were established that included the development of gastric cancer cell lines and the establishment of models of gastric carcinogenesis in non-human primates such as Sapajus apella. A co Read More

Chronic myeloid leukemia (CML) is a blood cancer predominantly affecting older adult patients. According to the American Cancer Society, an estimated 8,860 people will be diagnosed with CML in 2022. Treatments for CML have evolved with a focus on CML phase severity or progression. Overall, there have been some breakthrough treatment options for a high percentage of patients with CML. This is largely due to the dis Read More

The thiazolopyrimidine nucleus is a bioisosteric analog of purine and an important class of N-containing heterocycles. Thiazolopyrimidine scaffolds are considered a promising class of bioactive compounds that encompass diverse biological activities, such as antibacterial, antiviral, antifungal, anticancer, corticotrophin-releasing factor antagonists, anti-inflammatory, antituberculosis, and glutamic receptors antagonists. Despite Read More

Collagen is the most important structural protein and also the main component of the extra-cellular matrix (ECM). It plays a role in tumor progression. Collagen can be regulated by altering its biosynthesis pathway through various signaling pathways, receptors, and genes. The activity of cancer cells can also be regulated by other ECM components like metalloproteinases, hyaluronic acid, fibronectin, and so on. Hypoxia Read More

Background: Photodynamic therapy (PDT) is a therapeutic intervention that can be applied to cancer treatment. The interaction between a photosensitizer (PS), ideal wavelength radiation, and tissue molecular oxygen triggers a series of photochemical reactions responsible for producing reactive oxygen species. These highly reactive species can decrease proliferation and induce tumor cell death. The search for PS of nat Read More

Background: Artabotrys odoratissimus (Annonaceae) is a medicinal and ornamental plant widely cultivated in Southeast Asia for its famous ylang ylang essential oil. The fruits of this plant are used for health benefits, but very little is studied about the bioactive principles, their role in regulating oxidative stress and tumour progression. Objective: The study aimed to evaluate the antiproliferative effects of fruit extract of Artabotry Read More

Background: GRPR is over-expressed in cancer cells and is a potential drug target for the treatment of cancer. PD176252, as the most representative non-peptide inhibitor of GRPR, can inhibit the growth of cancer cells, but its low selectivity to cancer cells and normal cells limits its further application. Objective: The aim of this study was to design and synthesize novel GRPR inhibitor with stronger anti-cancer activity Read More

Background: DNA Topoisomerase II Alpha (TOP2A), a protein-coding gene, is central to the replication process and has been found deregulated in several malignancies, including breast cancer. Several therapeutic regimens have been developed and approved for targeting TOP2A and have prolonged the survival of cancer patients. However, due to the inherent nature of the tumor cell to evolve, the earlier positive response Read More

Background: Triple-negative breast cancer is challenging to treat due to its heterogeneity and lack of therapeutic targets. Hence, systemic chemotherapy is still the mainstay in TNBC treatment. Unfortunately, patients commonly develop chemoresistance. Androgen signalling through its receptor is an essential player in breast cancer, where it has been shown to confer chemoresistance to TNBC cells. Objective: The objec Read More