Polymers Based on Phenyl Boric Acid in Tumor-Targeted Therapy.

BACKGROUND: Tumors are still among the major challenges to human health. Tumor-targeted therapy is an effective way to treat tumors based on precise medical models. Sialic acid (SA) is overexpressed on the surface of tumor cells, and Phenyl Boric Acid (PBA) can specifically bind to SA. However, studies on the use of PBA in tumor-targeted therapy are few. OBJECTIVE: To summarize and analyze the characteristics and influencing factors of tumor targeted therapy in recent years, and the influencing factors of phenyl boric acid modified polymers in tumor targeted therapy, such as hydrogen ion concentration (pH), Adenosine Triphosphate (ATP), and sugars. This paper describes the application of phenyl boric acid partially functionalized nano-polymers in various types of targeted tumors, such as breast cancer, lung adenocarcinoma, liver cancer, and so forth. In order to further improve the basic research and clinical workers' understanding of nano-preparations and tumor targeted therapy. At the same time, it is also expected to promote the development value of phenyl boric acid. METHODS: The findings on tumor-targeted therapy and the role of partially functionalized polymers with PBA in different tumors at home and abroad has been analyzed and summarized in recent years. RESULTS: Tumor-targeted therapy is a promising treatment for tumors. PBA promotes the treatment of tumors using SA, which is highly expressed on the surface of tumor cells. CONCLUSION: Tumor-targeted therapy has shown great prospects for clinical application in recent years. PBA is beneficial as a member of the drug loading system. Further studies are still needed to promote its development and application.

Design, Synthesis, and Bioactivity of α-Ketoamide Derivatives Bearing a Vanillin Skeleton for Crop Diseases.

A series of novel α-ketoamide derivatives bearing a vanillin skeleton were designed and synthesized. Bioactivity tests on virus and bacteria were performed. The results indicated that some compounds exhibited excellent antitobacco mosaic virus (TMV) activities, such as compound 34 exhibited an inactivation activity of 90.1% and curative activity of 51.8% and compound 28 exhibited a curative activity of 54.8% at 500 µg mL-1, which is equivalent to that of the commercial ningnanmycin (inactivation of 91.9% and curative of 51.9%). Moreover, the in vitro antibacterial activity test illustrated that compounds 2, 22, and 33 showed much higher activities than commercial thiodiazole copper, which could be used as lead compounds or potential candidates. The findings of transmission electron microscopy and molecular docking indicated that the synthesized compounds exhibited strong and significant binding affinity to the TMV coat protein and could obstruct the self-assembly and increment of TMV particles. This study revealed that α-ketoamide derivatives bearing a vanillin skeleton could be used as a novel potential pesticide for controlling the plant diseases.

Novel anthranilic amide derivatives bearing the chiral thioether and trifluoromethylpyridine: Synthesis and bioactivity.

Ten anthranilic amides bearing skeletons of chiral thioether and trifluoromethylpyridine (5a-5j) were designed and synthesized. Bioassays indicated that some of compounds had excellent insecticidal activity. For example, compounds 5a, 5e and 5g had the median lethal concentrations (LC50) against Plutella xylostella of 7.3, 8.7 and 8.1 µg/mL respectively. The LC50 of 5a against Ostrinia nubilalis and Pseudaletia separata were 21.7 and 44.2 µg/mL respectively. Anti-TMV tests indicated that some compounds also showed good antiviral activity. For instance, the curative activities of compounds 5b and 5e were 57.2% and 63.6%, and with half maximal effective concentration (EC50) of 304.5 and 203.0 µg/mL, respectively, which were much higher than these of ribavirin (39.4%, EC50 = 819.8 µg/mL) and ningnanmycin (56.2%, EC50 = 361.4 µg/mL). The molecular docking between the most active compounds and ryanodine receptor of the Plutella xylostella were also discussed. Those results indicated that the novel anthranilic amide derivatives in present work were worthy of further research and development as novel pesticides.

Synthesis of Anthranilic Diamide Derivatives Containing Moieties of Trifluoromethylpyridine and Hydrazone as Potential Anti-Viral Agents for Plants.

A series of novel anthranilic diamide derivatives (5a-5ab) containing moieties of trifluoromethylpyridine and hydrazone was designed and synthesized. The synthesized compounds were evaluated in vivo for their activities against tobacco mosaic virus (TMV) and cucumber mosaic virus (CMV). Most of the synthesized compounds displayed good to excellent antiviral activities. The compounds 5i, 5k, 5s, 5w, 5x, and 5z had the curative activity over 65% against TMV at the concentration of 500 µg/mL, which were significantly higher than those of ningnanmycin (55.0%) and ribavirin (37.9%). Notably, the curative activity of compound 5i was up to 79.5%, with the EC50 value of 75.9 µg/mL, whereas the EC50 value of ningnanmycin was 362.4 µg/mL. The pot experiments also further demonstrated the significantly curative effect of 5i. Meanwhile, compounds 5h, 5p and 5x displayed more protective activities on TMV than that of ningnanmycin. Moreover, compounds 5a, 5e, 5f, and 5i showed inactivation activity similar to ningnanmycin at 500 µg/mL, and the EC50 value of 5e (41.5 µg/mL) was lower than ningnanmycin (50.0 µg/mL). The findings of transmission electron microscopic (TEM) indicated that the synthesized compounds exhibited strong and significant binding affinity to TMV coat protein (CP) and could obstruct the self-assembly and increment of TMV particles. Microscale thermophoresis (MST) studies on TMV-CP and CMV CP revealed that some of the active compounds, particularly 5i, exhibited a strong binding capability to TMV-CP or CMV-CP. This study revealed that anthranilic diamide derivatives containing moieties of trifluoromethylpyridine and hydrazone could be used as novel antiviral agents for controlling the plant viruses.

Pyrazolo[3,4-d]pyrimidine derivatives containing a Schiff base moiety as potential antiviral agents.

A series of pyrazolo[3,4-d]pyrimidine derivatives containing a Schiff base moiety were synthesized, characterised, and evaluated for their activity against tobacco mosaic virus (TMV). Biological assays indicated that several of the derivatives exhibited significant activity against TMV. In particularly, compounds 5y and 5aa displayed excellent inactivating activity against TMV, with half maximal effective concentration (EC50) values of 70.3 and 53.65 µg/mL, respectively, which were much better than that of ribavirin (150.45 µg/mL), and 5aa was superior to ningnanmycin (EC50 = 55.35 µg/mL). Interactions of compounds 5y and 5aa with TMV coat protein (TMV-CP) were investigated using microscale thermophoresis and molecular docking. Compounds 5y and 5aa displayed strong binding capability to TMV-CP with dissociation constant (Kd) values of 22.6 and 9.8 µM, respectively. These findings indicate that pyrazolo[3,4-d]pyrimidine derivatives containing a Schiff base may be potential antiviral agents.