The predominant impediments to cutaneous wound regeneration are hemorrhage and bacterial infections that lead to extensive inflammation with lethal impact. We thus developed a series of composite sponges based on polyvinyl alcohol (PVA) inspired by marjoram essential oil and kaolin (PVA/marjoram/kaolin), adopting a freeze–thaw method to treat irregular wounds by thwarting lethal bleeding and microbial infections. Microstructure analyses manifested three-dimensional interconnected porous structures for PVA/marjoram/kaolin. Additionally, upon increasing marjoram and kaolin concentrations, the pore diameters of the sponges significantly increased, recording a maximum of 34 ± 5.8 µm for PVA-M0.5-K0.1. Moreover, the porosity and degradation properties of PVA/marjoram/kaolin sponges were markedly enhanced compared with the PVA sponge with high swelling capacity. Furthermore, the PVA/marjoram/kaolin sponges exerted exceptional antibacterial performance against Escherichia coli and Bacillus cereus, along with remarkable antioxidant properties. Moreover, PVA/marjoram/kaolin sponges demonstrated significant thrombogenicity, developing high thrombus mass and hemocompatibility, in addition to their remarkable safety toward fibroblast cells. Notably, this is the first study to our knowledge investigating the effectiveness of marjoram in a polymeric carrier for prospective functioning as a wound dressing. Collectively, the findings suggest the prospective usage of the PVA-M0.5-K0.1 sponge in wound healing for hemorrhage and bacterial infection control.

In this study, an efficient multistep synthesis of novel aromatic tricyclic hybrids incorporating different biological active moieties, such as 1,3,4-thiadiazole and 1,2,4-triazole, was reported. These target scaffolds are characterized by having terminal lipophilic or hydrophilic parts, and their structures are confirmed by different spectroscopic methods. Further, the cytotoxic activities of the newly synthesized compounds were evaluated using in vitro MTT cytotoxicity screening assay against three different cell lines, including HepG-2, MCF-7, and HCT-116, compared with the reference drug Taxol. The results showed variable performance against cancer cell lines, exhibiting MCF-7 and HepG-2 selectivities by active analogs. Among these derivatives, 1,2,4-triazoles 11 and 13 and 1,3,4-thiadiazole 18 were found to be the most potent compounds against MCF-7 and HepG-2 cancer cells. Moreover, structure–activity relationship (SAR) studies led to the identification of some potent LSD1 inhibitors. The tested compounds showed good LSD1 inhibitory activities, with an IC₅₀ range of 0.04–1.5 μM. Compounds 27, 23, and 22 were found to be the most active analogs with IC₅₀ values of 0.046, 0.065, and 0.074 μM, respectively. In addition, they exhibited prominent selectivity against a MAO target with apparent cancer cell apoptosis, resulting in DNA fragmentation. This research provides some new aromatic-centered 1,2,4-triazole-3-thione and 1,3,4-thiadiazole analogs as highly effective anticancer agents with good LSD1 target selectivity.

Considering the widespread availability of certain medicines, there is still a critical need for potent anti-cancer agents. It is owing to numerous negative impacts and non-functionality of current drugs, particularly during the late stages of illness. To accomplish this, the new array of 1,2,3-triazole-benzothiazole molecular conjugates tethering hydrazone/thiosemicarbazone linkage 8a–l have been successfully synthesized via the efficient copper-catalyzed 1,3-dipolar cycloaddition of the appropriate un/substituted benzothiazole azides 4a–c with several O-propargylated benzylidene derivatives 7a–d. The newly established 1,2,3-triazole structural hybrids were thoroughly characterized using appropriate spectroscopic techniques (IR, ¹H, ¹³C-NMR & CHN analysis). The cytotoxic features of the investigated triazole hybrids were assessed against three human cancer cell lines, A549, T47-D, and HCT-116 cancer cells, using the MTT assay. Based on the findings, the breast cancer cell line T47D displayed promising results with IC₅₀ values of 13, 17, and 19 μM for the synthesized molecules 8a–c, respectively. Furthermore, the safety assessment of these compounds on normal cell lines revealed a relatively low risk to normal cells, as indicated by their IC₅₀ values exceeding 500 μM, suggesting a reasonable safety margin. Interestingly, the most relevant derivatives 8a, 8b, and 8c, exhibited IC₅₀ values of 0.69, 1.16, and 4.82 μM, respectively, causing inhibition of 98.5%, 96.8%, and 92.3%, compared to Erlotinib (IC₅₀ = 1.3 μM, 98.2% inhibition). Molecular docking results exhibited a good binding affinity of compounds 8a and 8b towards the EGFR active site. Accordingly, these compounds can be further developed as target-oriented EGFR chemotherapeutics against cancer.

In this work, we used microwave irradiation conditions to synthesize β-enaminonitrile (4), which was affirmed using single crystal X-ray diffraction and the different spectral data. Two tumor cell lines, MCF-7 and MCF-7/ADR, as well as two normal cell lines, HFL-1 and WI-38, were used to assess the anticancer activity of compound 4. The studied molecule exhibited potent efficacy against the MCF-7 and MCF-7/ADR cell lines compared with the reference drugs. Furthermore, target compound 4 had feeble activity against HFL-1 and WI-38. The chemical reactivity was discussed using DFT and QTAIM analysis to study the intrinsic electronic properties of compound 4. A molecular docking study was also conducted to examine their binding affinity to the EGFR. Compound 4 revealed a stable binding mode at the enzyme active pocket more than the reference inhibitor. The docking analysis was performed for molecule (4).

Polymer colloids have remarkable features and are gaining importance in many areas of research including medicinal science. Presently, the innovation of cancer drugs is at the top in the world. Polymer colloids have been used as drug delivery and diagnosis agents in cancer treatment. The polymer colloids may be of different types such as micelles, liposomes, emulsions, cationic carriers, and hydrogels. The current article describes the state-of-the-art polymer colloids for the treatment of cancer. The contents of this article are about the role of polymeric nanomaterials with special emphasis on the different types of colloidal materials and their applications in targeted cancer therapy including cancer diagnoses. In addition, attempts are made to discuss future perspectives. This article will be useful for academics, researchers, and regulatory authorities.

Some novel benzo[ d ]thiazole–1,2,3-triazole hybrid compounds with benzamide and/or benzoate tethers were synthesized as EGFR-dependent signaling inhibitors against breast cancer.