Quinazolinones, essential quinazoline derivatives, exhibit diverse biological activities with applications in pharmaceuticals and insecticides. Some derivatives have already been developed as commercial drugs. Given the rising cancer incidence, there is a critical need for new anticancer agents, and quinazolinones show promising potential in this domain. The present review focuses on novel advances in the synthesis of these important scaffolds and other medicinal aspects involving drug design, the structure–activity relationship, and action mechanisms of quinazoline and quinazolinone derivatives, to help in the development of new quinazoline and quinazolinone derivatives.

The feature of the PD-L1 protein and the basic backbone of PD-L1 small-molecule inhibitors have been summarized, it is an important guidance for researchers to develop PD-L1 small molecule inhibitors based on protein characteristic.

Iridoids, an important active ingredient, are widely distributed in varieties of Chinese herbal medicines and have varieties of pharmacological activities, such as anti-tumor, hypoglycemic, anti-inflammatory and so on, most of which exist in the form of glycosides in nature. However, its clinical application is limited by poor lipid solubility, low bioavailability and short half-life. It is necessary to optimize the structure of iridoids. It is hard to modify the hydroxyl groups at specific sites because iridoid glycosides are polyhydroxy compounds and very complex. In this paper, the words of ‘Iridoid glycosides’ and ‘Hydroxyl protection’ were used as the keywords, more than 200 articles from 1965 to 2021 were obtained from databases, such as CNKI, PubMed, Scifinder and so on. Finally, 60 articles were selected to summarize the hydroxyl protection of iridoid glycosides, which will provide a theoretical basis for their structural modification and stimulate their application potential in the field of drug research and development.

Catalpol and its derivatives were found in a variety of Chinese medicinal plants and possess various biological activities, such as anti‐inflammatory, anti‐oxidant, neuroprotective, cardiovascular protective, anti‐tumor and hypoglycemic and so on. The extensive pharmacological activities of catalpol have been attracted much attention to researchers, but the clinical applications are limited by poor lipid solubility, low bioavailability and short half‐life, so pharmacologists have made various structural modifications to catalpol, such as increasing lipid solubility to enhance its biological activities in the hope that it can be widely used in clinical applications. In this paper, using “Catalpol” and “Catalpol derivatives” as the keywords, more than 200 articles from 1965 to 2021 were obtained from databases, such as CNKI, PubMed, Scifinder and so on. Finally, 93 articles were selected to systematically analyze the structure and efficacy of catalpol and its derivatives according to pharmacological activity, which will provide ideas for the development of new catalpol drugs in the future.

This narrative review systematically evaluates the therapeutic potential and mechanisms of action of Arctii Fructus lignans (from Arctium lappa L.) in managing diabetes mellitus (DM) and its complications. To ensure a comprehensive evidence synthesis, a systematic literature search was conducted using PubMed, Web of Science, CNKI, and Wanfang Data for publications between January 2000 and June 2024. Study selection was based on predefined inclusion and exclusion criteria focusing on lignan-specific antidiabetic effects and mechanistic insights. The accumulated evidence demonstrates that Arctii Fructus lignans exhibit multi-targeted pharmacological effects through several key mechanisms: (1) improving glucose homeostasis via α-glucosidase inhibition and AMPK/PI3K pathway activation; (2) protecting pancreatic β-cell function through anti-inflammatory and anti-apoptotic actions; and (3) mitigating diabetic complications by reducing oxidative stress, modulating TGF-β/VEGF signaling, and restoring autophagy balance. Notably, these lignans show particular efficacy in early-stage diabetes models, with reduced effectiveness in advanced stages featuring significant β-cell dysfunction, suggesting a critical therapeutic window for intervention. Future research should prioritize well-designed clinical trials using standardized extracts, investigations into structure–activity relationships, and exploration of synergistic effects within traditional formulations to advance the translational potential of these promising natural compounds.