This study investigates the anti-proliferative potential and possible molecular mechanisms of 3-(2-furoyl)-indole derivatives against HepG2.

The review discusses progress in discovering cyclin-dependent kinase 2 (CDK2) inhibitors for cancer treatment and their potential for male contraception. It summarizes first-, second-, and third-generation CDK inhibitors and selective CDK2 inhibitors currently in clinical trials for cancer. Novel strategies to discover allosteric inhibitors, covalent inhibitors, and degraders are also discussed.

Type-2 diabetes mellitus (T2DM) is a major metabolic disorder needing insulin-independent treatments; this study developed Schiff base 1,3,4-thiadiazole as Sodium Glucose Co-transporters 2 (SGLT2) inhibitors.

Peptides are able to bind to difficult disease targets with high potency and specificity, providing great opportunities to meet unmet medical requirements. Nevertheless, the unique features of peptides, such as their small size, high structural flexibility, and scarce data availability, bring extra challenges to the design process. Firstly, this review sums up the application of peptide drugs in treating diseases. Then, the review probes into the advantages of Deep Neural Networks (DNNs) in predicting and designing peptide structures. DNNs have demonstrated remarkable capabilities in structural prediction, enabling accurate three-dimensional modeling of peptide drugs through models like AlphaFold and its successors. Finally, the review deliberates on the challenges and coping strategies of DNNs in the development of peptide drugs, along with future research directions. Future research directions focus on further improving the accuracy and efficiency of DNN-based peptide drug design, exploring novel applications of peptide drugs, and accelerating their clinical translation. With continuous advancements in technology and data accumulation, DNNs are poised to play an increasingly crucial role in the field of peptide drug development.

8-Hydroxyquinoline and 4-thiazolidinone derivatives are promising antimicrobial agents, recognized for their activity against resistant pathogens.

Trypanosomatid diseases, leishmaniasis and trypanosomiasis are vector-borne parasitic diseases that can cause death and catastrophic economic losses for millions of people. The growing resistance of trypanosomatid parasites to current treatments highlights the urgent need for new therapeutic agents. This study explored 5-nitroindole-rhodanine conjugates to identify promising new compounds with the potential for future development as antitrypanosomatid treatments.

New triazoloquinazoline derivatives were synthesized to explore their cytotoxic activity on various cancer cell lines, prompted by the need for effective anticancer agents.

This work explores the synthesis of new bi-heterocyclic hybrid compounds based on quinoline ring and investigates their potential as anticancer agents.

Neurodegenerative diseases are characterized by impairments in movement and cognitive functions. These disorders are frequently associated with the accumulation of misfolded protein aggregates, which present significant challenges for treatment with conventional small-molecule inhibitors. While FDA-approved amyloid-beta-directed antibodies, such as Lecanemab, have recently shown clinical success in modifying disease progression, there are currently no treatments capable of curing neurodegenerative diseases. Emerging technologies like proteolysis-targeting chimeras (PROTACs) offer additional promise by targeting disease-causing proteins for degradation, potentially opening new therapeutic avenues. Recent experiments have demonstrated that PROTACs can specifically target and degrade pathogenic proteins associated with neurodegenerative diseases, thereby offering potential therapeutic avenues. This review discusses the latest advances in employing PROTACs for treating neurodegenerative diseases and delves into the associated challenges and opportunities. Our goal is to provide researchers in drug development with new insights on creating novel PROTACs for therapeutic applications.

The advancement of targeted drug delivery systems has opened up a wide array of opportunities in cancer therapy, leading to the exploration of various strategies. Among these, the use of prodrugs stands out as a particularly promising approach in targeted cancer treatment, aimed at enhancing the selectivity and effectiveness of cytotoxic agents. In the last few years, there has been considerable progress in the area of dimeric-based prodrugs aimed at cancer therapy. The advantages presented by dimeric-based prodrugs have significantly improved the efficiency of delivering anticancer drugs, characterized by a high drug loading capacity, advantageous pharmacokinetics, and drug release that responds to tumor stimuli. With respect to the importance of drug dimerization in the field of prodrug development, herein we review the latest reports covering research in dimeric prodrugs. We have categorized the article according to the reported anticancer agents. We have also spent a great deal of attention on different types of used linkers and methods of the dissociation of dimeric prodrugs into free monomeric drugs. Readers will easily be able to compare between the reported research using the same drugs with different linkers or different dissociation methods as well as different cancer cell lines targeted in the studies.

The globally growing antimicrobial resistance seriously threatens human health, increasing efforts have been devoting to the development of novel antibiotics. Naphthalimides contain a special skeleton of cyclic double imides and the naphthalene framework, this unique structure can exert multitargeting abilities which are helpful to overcome the escalating issue of resistance. Therefore, research in connection with the development of naphthalimides as novel antimicrobial agents is becoming progressively active. It has been revealed that naphthalimides as novel structural skeleton of multitargeting promising antibiotics could not only target DNAs and enzymes, disturb membrane, produce reactive oxygen species, . suggesting the multitargeting actions which do not induce resistance, but also show a broad antimicrobial spectrum with safety profile and pharmacokinetic characteristics, implying large potential as a new type of antibiotics continuous efforts toward antimicrobial naphthalimides. This review presents naphthalimides as a new type of potential antimicrobial agents and discusses rational design strategies, structure-activity relationships, and mechanisms of action, with a comprehensive view to providing a new insight for in the rational design of efficient, broad-spectrum, and low-toxic naphthalimide antibiotics.

Drug-loaded poly(lactic-co-glycolic acid) (PLGA) scaffolds were fabricated using a mold-less technique to investigate whether the combined delivery of both Y15 (FAK inhibitor) and metformin would result in enhanced effects on cell viability compared to the release of each drug alone for the treatment of platinum-resistant ovarian cancer (PROC).

Upregulation of Cyclooxygenase-2 (COX-2) in a variety of cancer cell lines, a key enzyme of prostaglandin biosynthesis, relative to surrounding normal tissues results in the use of the COX-2 protein as an attractive molecular target for many anticancer therapeutics. This could have a significant implication for selective destruction of cancer cells via the photodynamic therapy effects, leaving the normal tissue intact.