Current Topics in Medicinal Chemistry - Volume 24, Issue 7, 2024

The signal transduction and cell proliferation are regulated by the epidermal growth factor receptor. The proliferation of tumor cells, apoptosis, invasion, and angiogenesis is inhibited by the epidermal growth factor receptor. Thus, breast cancer, non-small cell lung cancer, cervical cancer, glioma, and bladder cancer can be treated by targeting the epidermal growth factor receptor. Although third-generation epidermal growth factor receptor inhibitors are potent drugs, patients exhibit drug resistance after treatment. Thus, the search for new drugs is being continued. Among the different potent epidermal growth factor receptor inhibitors, we have reviewed the indole-based inhibitors. We have discussed the structure-activity relationship of the compounds with the active sites of the epidermal growth factor receptor receptors, their synthesis, and molecular docking studies.

COVID-19, stemming from SARS-CoV-2, poses a formidable threat to global healthcare, with a staggering 77 million confirmed cases and 690,067 deaths recorded till December 24, 2023. Given the absence of specific drugs for this viral infection, the exploration of novel antiviral compounds becomes imperative. High-throughput technologies are actively engaged in drug discovery, and there is a parallel effort to repurpose plant-based molecules with established antiviral properties. In this context, the review meticulously delves into the potential of plant-based folk remedies and existing molecules. These substances have showcased substantial viral inhibition in diverse in vivo, in silico, and in vitro studies, particularly against critical viral protein targets, including SARS-CoV-2. The findings position these plant-based molecules as promising antiviral drug candidates for the swift advancement of treatments for COVID-19. It is noteworthy that the inherent attributes of these plant-based molecules, such as their natural origin, potency, safety, and cost-effectiveness, contribute to their appeal as lead candidates. The review advocates for further exploration through comprehensive in vivo studies conducted on animal models, emphasizing the potential of plant-based compounds to help in the ongoing quest to develop effective antivirals against COVID-19.

Osteoporosis and other bone diseases are a major public health concern worldwide. Current pharmaceutical treatments for bone disorders have limitations, driving interest in complementary herbal medicines that can help maintain bone health. This review summarizes the scientific evidence for medicinal herbs that modulate bone cell activity and improve bone mass, quality and strength. Herbs with osteogenic, anti-osteoporotic, and anti-osteoclastic effects are discussed, including compounds and mechanisms of action. Additionally, this review examines the challenges and future directions for translational research on herbal medicines for osteoporosis and bone health. While preliminary research indicates beneficial bone bioactivities for various herbs, rigorous clinical trials are still needed to verify therapeutic efficacy and safety. Further studies should also elucidate synergistic combinations, bioavailability of active phytochemicals, and precision approaches to match optimal herbs with specific etiologies of bone disease. Advancing evidence- based herbal medicines may provide novel alternatives for promoting bone homeostasis and treating skeletal disorders.

Background: The concept of utilizing drug repurposing/repositioning in the development of hybrid molecules is an important strategy in drug discovery. Fluoroquinolones, a class of antibiotics, have been reported to exhibit anticancer activities. Although anticancer drug development is achieving some positive outcomes, there is still a need to develop new and effective anticancer drugs. Some limitations associated with most of the available anticancer drugs are drug resistance and toxicity, poor bio-distribution, poor solubility, and lack of specificity, thereby reducing their therapeutic outcomes. Objectives: Fluoroquinolones, a known class of antibiotics, have been explored by hybridizing them with other pharmacophores and evaluating their anticancer activity in silico and in vitro. Hence, this review provides an update on new anticancer drugs containing fluoroquinolones moiety, Ciprofloxacin and Norfloxacin between 2020 and 2023, their structural relationship activity, and the future strategies to develop potent chemotherapeutic agents. Methods: Fluoroquinolones were mostly hybridized via the N-4 of the piperazine ring on position C-7 with known pharmacophores characterized, followed by biological studies to evaluate their anticancer activity. Results: The hybrid molecules displayed promising and interesting anticancer activities. Factors such as the nature of the linker, the presence of electron-withdrawing groups, nature, and position of the substituents influenced the anticancer activity of the synthesized compounds. Conclusion: The hybrids were selective towards some cancer cells. However, further in vivo studies are needed to fully understand their mode of action.