A notable increase in cancer-related fatalities and morbidity worldwide is attributed to drug resistance. The factors contributing to drug resistance include drug efflux via ABC transporters, apoptosis evasion, epigenetic alterations, DNA repair mechanisms, and the tumor microenvironment, among others. Systemic toxicities and resistance associated with conventional cancer diagnostics and therapies have led to the development of alternative approaches, such as nanotechnology, to enhance diagnostic precision and improve therapeutic outcomes. Nanomaterial, including carbon nanotubes, dendrimers, polymeric micelles, and liposomes, have shown significant benefits in cancer diagnosis and treatment due to their unique physicochemical properties, such as biocompatibility, stability, enhanced permeability, retention characteristics, and targeted delivery. Building on these advantages, this review is conducted through comprehensive analysis of recent literature to explore the principal mechanisms of drug resistance, the potential of nanomaterials to revolutionize selective drug delivery and cancer treatment. Additionally, the strategies employed by nanomaterials to overcome drug resistance in tumors, such as efflux pump inhibition, multidrug loading, targeted delivery to the tumor microenvironment, and gene silencing therapies are discussed in detail. Furthermore, we examine the challenges associated with nanomaterials that limit their application and impede their transition to clinical use.

A series of symmetrical salicylaldehyde-bishydrazine azo molecules, 5a–5h, have been synthesized, characterized by ¹H-NMR and ¹³C-NMR, and evaluated for their in vitro α-glucosidase and α-amylase inhibitory activities. All the synthesized compounds efficiently inhibited both enzymes. Compound 5g was the most potent derivative in the series, and powerfully inhibited both α-glucosidase and α-amylase. The IC₅₀ of 5g against α-glucosidase was 0.35917 ± 0.0189 µM (standard acarbose IC₅₀ = 6.109 ± 0.329 µM), and the IC₅₀ value of 5g against α-amylase was 0.4379 ± 0.0423 µM (standard acarbose IC₅₀ = 33.178 ± 2.392 µM). The Lineweaver-Burk plot indicated that compound 5g is a competitive inhibitor of α-glucosidase. The binding interactions of the most active analogues were confirmed through molecular docking studies. Docking studies showed that 5g interacts with the residues Trp690, Asp548, Arg425, and Glu426, which form hydrogen bonds to 5g with distances of 2.05, 2.20, 2.10 and 2.18 Å, respectively. All compounds showed high mutagenic and tumorigenic behaviors, and only 5e showed irritant properties. In addition, all the derivatives showed good antioxidant activities. The pharmacokinetic evaluation also revealed promising results

Sulfonamide derivatives serve as an important building blocks in the drug design discovery and development (4D) process. Ciprofloxacin-, sulfadiazine- and amantadine-based sulfonamides were synthesized as potent inhibitors of jack bean urease and free radical scavengers. Molecular diversity was explored and electronic factors were also examined. All 24 synthesized compounds exhibited excellent potential against urease enzyme. Compound 3e (IC₅₀ = 0.081 ± 0.003 µM), 6a (IC₅₀ = 0.0022 ± 0.0002 µM), 9e (IC₅₀ = 0.0250 ± 0.0007 µM) and 12d (IC₅₀ = 0.0266 ± 0.0021 µM) were found to be the lead compounds compared to standard (thiourea, IC₅₀ = 17.814 ± 0.096 µM). Molecular docking studies were performed to delineate the binding affinity of the molecules and a kinetic mechanism of enzyme inhibition was propounded. Compounds 3e, 6a and 12d exhibited a mixed type of inhibition, while derivative 9e revealed a non-competitive mode of inhibition. Compounds 12a, 12b, 12d, 12e and 12f showed excellent radical scavenging potency in comparison to the reference drug vitamin C.

A small library of new drug-1,3,4-thiazidazole hybrid compounds (3a–3i) was synthesized, characterized, and assessed for their acetyl cholinesterase enzyme (AChE) inhibitory and free radical scavenging activities. The newly synthesized derivatives showed promising activities against AChE, especially compound 3b (IC₅₀ 18.1 ± 0.9 nM), which was the most promising molecule in the series, and was substantially more active than the reference drug (neostigmine methyl sulfate; IC₅₀ 2186.5 ± 98.0 nM). Kinetic studies were performed to elucidate the mode of inhibition of the enzyme, and the compounds showed mixed-type mechanisms for inhibiting AChE. The Ki of 3b (0.0031 µM) indicates that it can be very effective, even at low concentrations. Compounds 3a–3i all complied with Lipinski’s Rule of Five, and showed high drug-likeness scores. The pharmacokinetic parameters revealed notable lead-like properties with insignificant liver and skin-penetrating effects. The structure–activity relationship (SAR) analysis indicated π–π interactions with key amino acid residues related to Tyr124, Trp286, and Tyr341.

Background Pakistan has already encountered intense opposition to polio vaccination due to myths and misinformation, now the unfavorable opinions of COVID-19 vaccinations among the population would have catastrophic consequences for attempts to end the pandemic. Methods A web-based cross-sectional study was conducted in the general population of Sindh, Pakistan in January 2021. 31 items based on vaccines availability, safety, and myths, the questionnaire was designed and randomly distributed through a google form link. Results were analyzed using descriptive and Chi-square tests. Results A total of 774 responses were recorded from 23 districts of Sindh, Pakistan. The majority of participants (n=00, 00.0%) were not aware of the presence of the COVID-19 vaccine in Pakistan. Results found the significant relationship of conspiracies and myths with an education level of participants, to make Muslims infertile, illiterate showed (Yes n=45, No=27) while postgraduate (Yes n=11, No=88) (χ2 = 109.6, P> 0.000). Participants showed doubt about the safety of vaccines, (Yes n= 464, 59.9%, No= 310, 40.1%). Other responses related to side effects of the vaccine were also highly significant, participants showed that vaccine side effects (Yes n= 462, 59.7%, No= 312, 40.3%), Pregnant or breastfeeding women should not get vaccinated (Yes n= 468, 59.8%, No= 311, 40.1%) and people with underlying conditions should not get vaccinated (True n= 389, 50.3%, False= 385, 49.7%). Conclusion The proportion of varying public doubts in vaccines’ safety and efficacy and the presence of myths, conspiracies will be a major barrier to vaccine uptake.