Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 23, Issue 4, 2023

Glioblastoma is an aggressive and recurrent tumour that affects our brain and spinal cord with an extensively poor prognosis and death of the patient within 14-15 months of diagnosis. The tumour originates from astrocytes and therefore comes under the glioma known as astrocytoma. These tumours exhibit miscellaneous properties and contain cancer stem cells (CSCs). The stem cells exhibit diverse mechanisms throu Read More

Cyclin Dependent Kinase 9 (CDK9), which controls transcriptional elongation, is a promising pharmacological target for a variety of cancerous cells, specifically those characterized by transcriptional dysregulation. CDK9 promotes the pause or release of RNA polymerase II, a rate-limiting stage in normal transcriptional regulation that is often disturbed in cancers. New indications suggest that selective CDK9 antagonism may be ben Read More

Cancer is becoming a global threat as its treatment accounts for many challenges. Hence, newer inventions prioritize the requirement of developing novel anticancer agents. In this context, kinases have been exclusively investigated and developed as a promising and novel class of drug targets for anticancer regimen. Indole derivatives have been found to be most effective for targeting multiple kinases, such as PIM, Read More

Flavonoid metal ion complexes are one of the classes of biologically active molecules with immense pharmacological potential, including antioxidant, antidiabetic, antimicrobial, and anticancer activity, to name a few. The effectiveness of this complexion depends on the state and nature of the transition metal ions and on the position to which the metal ion coordinates with their corresponding parent flavonoid. The Read More

Abstract: Aim: The study aims to investigate the combined effects of chrysin and cisplatin on hepatoma(HepG2) cell lines in vivo and in vitro. Objective: Studies have suggested that chrysin can enhance the sensitivity of tumor cells to apoptosis. Drug resistance in tumor cells reduced the effectiveness of chemotherapy drugs such as cisplatin. We investigated whether the combination of chrysin and cisplatin can induce mo Read More

Background: In-depth and clear mechanistic study is a prerequisite for new drugs to enter clinical research. Methods: New chemical entity BY4008 was identified by our lab as a novel and highly potent EGFR and JAK3 dualtarget inhibitor. A cell-based test exhibited strong antiproliferative activities against SW620 and HCT116 colon cancer cells harboring KRAS mutation with IC50 of nanomolar potency. Furthermore, acridin Read More

Aims: To find out the role of secretory phospholipase A2 (sPLA2) isozymes as potential targets in tobacco condensate-induced colon damage. Background: The effects of cigarette smoke condensate (CSC) and the molecular mechanisms involved in the regulation of phospholipase A2 (PLA2) and its isozymes in colon cells, which are still unclear and emerging, are studied. Objectives: The study aimed to check the effect of CSC Read More

Purpose: To investigate the safety and efficacy of lobaplatin-TACE in treating primary hepatocellular carcinoma. Methods: The data of 536 patients who underwent TACE in the interventional department from January 2016 to January 2020 were collected. Patients were divided into two groups according to the chemotherapeutic drugs used in TACE.: the epirubicin-TACE group (N = 260) and the lobaplatin-TACE group (N = 276). Read More

Background: Triple-negative breast cancer (TNBC) is considered to be the most malignant subtype of breast cancer (BC). Heparanase (HPSE) has been reported to contribute to tumor development, but its potential function in TNBC is not clear. The intention of this study was to investigate whether HPSE affects TNBC progression and to explore the possible mechanisms. Methods: Bioinformatics analyses were applied to anal Read More

Background: Aesculetin (AE), a natural coumarin derivative found in traditional medicinal herbs, has a variety of pharmacological effects. However, the role of AE and its molecular mechanisms of action on bladder cancer remains undefined. Objective: The study aims to explore the anti-tumor effects of AE on bladder cancer cells and the associated molecular mechanisms. Methods: We performed a Cell Counting Kit-8 assay to Read More