Current Medicinal Chemistry - Volume 31, Issue 5, 2024

Imidazo[4,5-b]pyridines are amongst the oldest known heteroaromatic derivatives. Their structural similarity with purine basis has however aroused the curiosity of biologists and resulted in the developments of innovative bioactive compounds. This review thus firstly describes the main synthetic ways currently used to produce imidazo[ 4,5-b]pyridine derivatives, and secondly gives examples of their potential, especially focusing o Read More

Background: Sesquiterpene lactones are secondary plant metabolites with a wide variety of biological activities. The process of lactone conjugation to other pharmacophores can increase the efficacy and specificity of the conjugated agent effect on molecular targets in various diseases, including brain pathologies. Derivatives of biogenic indoles, including neurotransmitter serotonin, are of considerable interest as potenti Read More

Cancer is a complex and debilitating disease that is one of the leading causes of death in the modern world. Computational methods have contributed to the successful design and development of several drugs. The recent advances in computational methodology, coupled with the avalanche of data being acquired through high throughput genomics, proteomics, and metabolomics, are likely to increase the contribut Read More

Background: Breast cancer (BC) is one of the most typical causes of cancer death in women worldwide. Activated epidermal growth factor receptor (EGFR) signaling has been increasingly associated with BC development and resistance to cytotoxic drugs. Due to its significant association with tumour metastasis and poor prognosis, EGFR-mediated signaling has emerged as an attractive therapeutic target in BC. Mainly in all BC Read More

Background: Epidermal growth factor receptor (EGFR/HER-1) and its role in tumor development and progression through the mechanism of tumor angiogenesis is prevalent in non-small lung cancer, head and neck cancer, cholangiocarcinoma & glioblastoma. Previous treatments targeting the oncogenic activity of EGFR's kinase domain have been hindered by acquired mutational resistance and side effects from existing drugs li Read More

Background: As a part of our discovery of plant-based lead molecules, we provide a helpful tool, which helps in identification, designing, optimising, structural modifications, and prediction of curcumin, to discover novel analogs with enhanced bioavailability, pharmacologically safe, and anticancer potential. Methods: QSAR (Quantitative structure-activity relationship) and pharmacophore mapping models were developed Read More

Background: Free radicals exist as unstable and highly reactive substances, occurring both in and outside the body. Free radicals are labeled as electron-hungry molecules formed from metabolism and endogenous burning of oxygen. They are transported in cells, upsetting the arrangement of molecules and instigating cellular injury. Hydroxyl radical (•OH) is one of the highly reactive free radicals, which damages the biomole Read More

Background: Breast cancer is the leading cause of cancer-related mortality among women worldwide. Advanced stages are usually obstinate with chemotherapy, resulting in a poor prognosis; however, they are treatable if diagnosed early. Objective: Identifying biomarkers that can detect cancer early or have therapeutic significance is imperative. Methods: Herein, a comprehensive bioinformatics-based transcriptomics stu Read More