Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 23, Issue 7, 2023

Purpose: The Warburg effect is an important metabolic feature of tumours, and hexokinase is the first ratelimiting enzyme of the glycolytic pathway during tumour metabolism. Among hexokinase subtypes, hexokinase 2 (HK2) is increasingly proving to be a key target for cancer treatment. This study presents the challenges and potential strategies for developing HK2 inhibitors by systematically summarising the characteristics of Read More

Bakuchiol is a meroterpene natural product distributed in various plants. It possesses several biological activities particularly anticancer. A large number of analogs have been prepared by various researchers by targeting several positions such as phenolic –OH, ethenyl and isopropylidene groups present in the bakuchiol to develop potent therapeutic agents with improved pharmaceutical properties. The present review des Read More

Historically, natural plant-derived drugs received a great impact of consideration in the treatment of several human-associated disorders. Cancer is a devastating disease and the second most cause of mortality. Sanguinarine (SANG), a naturally isolated plant alkaloidal agent, possesses chemo-preventive effects. Several studies have revealed that SANG impedes tumor metastasis and development by disrupting a wide range of Read More

Background: Cancer is associated with metabolic changes from increased cell proliferation and growth. Compared to normal differentiated cells, MM cells use the glycolytic pathway even when adequate oxygen is present triggering “Glutamine addiction”. Objective: To investigate the single and combined effects of epigallocatechin-3-gallate (EGCG) and telaglenastat, a glutaminase inhibitor, on the proliferation and apoptosis Read More

Purpose: The study aims to investigate the suppressing tumor-promoting effects via multi-anti-angiogenesis activity of the copper chelator (ammonium tetrathiomolybdate, TM) combined with lenvatinib for hepatocellular carcinoma. Methods: A total of 55 C57 mice were injected subcutaneously with Hepa1-6 hepatoma cell suspensions into the right posterior thigh. After 7 days, the subcutaneous tumors were for Read More

Background: As epigenetic readers, Bromodomain and extraterminal domain (BET) proteins have attracted immense interest in developing novel therapies targeting this family to inhibit cancer progression. Although the impact of BRD4 in the carcinogenesis of various tumors has been widely investigated, little is known about the potential roles of the BET family in gastric cancer. Methods: In this cohort study, we have screened Read More

Background: Renal cell carcinoma (RCC) is a common malignant tumor of the urinary system with a high recurrence rate and easy metastasis. Current clinical drugs for renal cell carcinoma include immunotherapies and targeted drugs. Axitinib is a clinically targeted drug for treating renal cell carcinoma, which has shortcomings such as unstable efficacy and easy drug resistance. Therefore, this study aims to determine wh Read More

Aims: The aim of this study was to sensitize the resistant breast adenocarcinoma cells towards Tumour Necrosis Factor-related Apoptosis-inducing Ligand (TRAIL)-induced apoptosis. Background: Breast cancer is a heterogeneous disease involving complex mechanisms. TRAIL is a potential anticancer candidate for targeted treatment due to its selective killing effects on neoplastic cells. Nonetheless, resistance occurs in man Read More

Background: Various natural products have been demonstrated for their anti-tumor activities. As a natural triterpenoid, the effects of ganoderic acid A on oxaliplatin chemotherapy for cancer treatment remain unclear. Methods: A xenograft mouse model of colon cancer was constructed using the HT-29 cells. Ganoderic acid A was intravenously administered with or without oxaliplatin. The CCK-8 method was performed to Read More

Background: Rhodanine derivatives have a proven wide range of biological activities. Objective: The aim of this study was to evaluate the cytotoxic effect of a series of rhodanine derivatives and investigate the quantitative structure-activity relationships, as well as binding modes to tyrosine kinase. Methods: Cytotoxic effect on cell proliferation (CaCo-2, HeLa, MDCK-1, Hut-78, K562) in vitro was evaluated by the MTT viability a Read More

Background: Galangin is one of the flavonoids in Alpinia officinarum. It has various anti-tumor activities, but its anti-bladder cancer effect is unclear. Objective: To investigate the mechanism of action of galangin against bladder cancer using a network pharmacology approach. Methods: The TCM Systematic Pharmacology Database and Analysis Platform (TCMSP), SwissTargetPrediction database, and the Targetnet database were u Read More