The rising prevalence of multidrug-resistant pathogens and the global burden of cancer necessitate the development of new therapeutic agents using sustainable, innovative approaches. Pyrimidine derivatives have attracted considerable attention due to their diverse biological activities, including antimicrobial and anticancer properties. Despite numerous reports on their synthesis, a clear gap remains in the literature regarding green synthesis protocols that combine eco-friendly reaction conditions with comprehensive biological and computational evaluations. In this work, we report a sustainable synthesis of these compounds using both conventional and microwave-assisted methods. Furthermore, we provide detailed characterization and in vitro assessments of biological activity. Compounds 7c, 8c, and 10a showed promising results, while extensive computational studies (DFT, molecular docking, and MD simulations) were conducted to elucidate the structure–activity relationships. This integrated approach not only deepens understanding of the pharmacological potential of these compounds but also aligns with the principles of green chemistry, offering a promising pathway for future drug discovery.
To explore more potential fungicides with new scaffolds, 10 norbornene derivatives containing thiourea group were designed, synthesized and assayed for inhibitory activity against three plant pathogenic fungi. The preliminary antifungal assay suggested that the title derivatives showed moderate to good antifungal activity against six plant pathogens. Especially, norbornene derivatives 3g presented excellent in vitro antifungal activity against Botryosphaeria dothidea (EC50 = 9.51 mg/L), which was approached to chlorthalonil. In vivo antifungal assay indicated norbornene derivatives 3g displayed excellent protective and curative effects on apple fruits infected by B. dothidea. The preliminary mechanism study displayed that norbornene derivatives 3g could damage the surface morphology. In addition, the phytotoxicity test revealed norbornene derivatives 3g showed safety on seeds of mung bean. The bioassay results and mechanism investigation demonstrated that this class of norbornene derivatives containing thiourea group could be promising fungicide for further development.
In face of large-scale plant diseases, the control of chemical pesticides remained a fast, economical and effective method. The search for novel bioactive pesticide has long been a priority in crop protection for solve the plant pathogen resistance. Natural products and their derivatives have been the major sources of the discovery of novel fungicides. Succinate dehydrogenase inhibitors (SDHIs) fungicides are the third largest category of fungicides. Meanwhile, the resistance of SDHIs with plant pathogen had been an urgent problem. It was an effective way to delay the resistance problem by the creation of fungicides from natural product. Considering these issues, here we have reviewed the published articles on the SDHIs fungicides during past five years (2020–2024) based on three kinds of natural product scaffolds.
Chiral γ-nitroketone-derived pyrrolidine N-oxide (III) exhibited potent in vitro anti-tumor activity against three cancer cell lines: human breast carcinoma (MDA-MB-231), human colorectal carcinoma (SW-480), and murine colorectal carcinoma (CT-26), with IC50 values of 8.81 ± 0.12 μM, 9.07 ± 0.31 μM, and 5.68 ± 0.10 μM, respectively. Informed by the findings, a series of quinoline-derived chiral γ-nitroketones were synthesized via an efficient organocatalytic asymmetric strategy, achieving excellent yields (up to 99 %) and enantioselectivities (up to 99 % ee). This synthetic strategy involves enantioselective Michael additions between nitroalkanes and 2-enoylquinolines, catalyzed by a bifunctional squaramide under solvent-free conditions.
A novel series of triazolothiadiazines has been successfully synthesized with high efficiency through Knoevenagel condensation, utilizing thiocarbamoyl dihydrazine as the starting material. The structures of these compounds were characterized through 1 H-NMR, 13 C-NMR, high-resolution mass spectrometry. The MTT assay was utilized to evaluate the in vitro cytotoxicity of the synthesized compounds against four human cancer cell lines including SW620, A549, Hela, and MCF-7. Among the tested compounds, (Z)-3-methyl-6-phenyl-7-(3-(trifluoromethyl)benzylidene)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine exhibited notably potent antiproliferative activity against all four human cancer cell lines.
