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Relevant academic research and scientific papers

Synthesis and antiviral bioactivity of novel chalcone derivatives containing purine moiety

A series of novel chalcone derivatives containing purine moiety was designed and synthesized, and their antiviral activities against cucumber mosaic virus (CMV) and tobacco mosaic virus (TMV) were evaluated in vivo. Bioactivity assays indicated that some compounds showed good antiviral activities against CMV and TMV. It is worth mentioning that compounds 3o, 3s, 3w, and 3x exhibited excellent curative activity against CMV, with EC50 values of 301.1 μg/mL, 315.7 μg/mL, 282.3 μg/mL, 230.5 μg/mL, respectively, which were better than that of Dufulin (373.7 μg/mL) and Ribavirin (726.3 μg/mL). In addition, the fluorescence spectroscopy experiment results showed that compound 3o showed strong combining capacity to tobacco mosaic virus coat protein.

4-[3-(3,4-dimethoxyphenyl)prop-2-enoyl]phenyl methacrylate and 4-[3-(2-bromophenyl)prop-2-enoyl]phenyl methacrylate.

Chalcones (alpha,beta-unsaturated ketones) are effective antitumour agents. It has been proved that having halogen or methoxy groups substituted in various positions of the phenyl ring enhances the activity of chalcones many times. The title compounds, C2

Synthesis and anticancer activity of chalcone–quinoxalin conjugates

Two series of quinoxaline–chalcone conjugates have been prepared by aldolic condensation and aromatic nucleophilic substitution reaction, and their anticancer activity against three cancer cell lines including benign prostatic hyperplasia epithelial cell (BPH-1), neuron-like rat pheochromocytoma cell line (PC12) and human breast cancer cell line (MCF-7) were evaluated in?vitro. All of the synthesized compounds exhibited moderate to good activity against the cancer cell lines selected. Particularly, Compound A5 showed the excellent potent activity against BPH-1 and MCF-7 with IC50 values of 10.4 and 9.1 μM, respectively, which is similar to doxorubicin (14.1 and 9.2 μM, respectively). As well as compound B6 exhibited most excellent activity toward PC12 with IC50 values of 16.4 μM. Compound A10 exhibited 55.4, 36.8 and 54.5 folds higher selectivity for BPH-1, PC12 and MCF-7 cells than for HEK-293 cell, respectively. In addition, theoretical biological activities of compounds A5 and A10 were evaluated by SwissADME.

Pyridine-containing benzothiazepine derivatives, and preparation method and application thereof

The invention discloses pyridine-containing benzothiazepine derivatives, and a preparation method and application thereof. The general formula (I) of the derivatives is described in the specification. In the formula (I), R is selected from a group consisting of a phenyl group, a 4-methylphenyl group, a thien-2-yl gourp, a 4-methoxyphenyl group, a 4-nitrophenyl group, a 4-trifluoromethoxyphenyl group, a 4-bromophenyl group, a furan-2-yl group, a 4-fluorophenyl group, a 3,4-dimethyoxyphenyl group, a 2-chlorophenyl group, a 2-phenyl group, a 3-bromophenyl group, a 2-methyoxyphenyl group, a 2-fluorophenyl group, a 3-methyoxyphenyl group, a 4-trifluoromethylphenyl group, a 2-trifluoromethylphenyl group, a 4-chlorophenyl group, a 3-fluorophenyl group, a 2,4-dichlorophenyl group, a 3,4-dichlorophenyl group, a 2,6-dichlorophenyl group, a 2-chloro-6-fluorophenyl group, a 3-nitrophenyl group and a naphtha-1-yl group. According to the invention, synthesis route is simple; yield is high; and plant virus diseases can be efficiently and safely prevented and controlled.

Synthesis and fungicidal evaluation of novel chalcone-based strobilurin analogues

Strobilurin derivatives have become one of the most important classes of agricultural fungicide due to a novel action mode, wide fungicidal spectrum, lower toxicity toward mammalian cells, and environmentally benign characteristics. To discover new strobilurin analogues with high activity against resistant pathogens, a series of new chalcone-based strobilurin derivatives are designed and synthesized by integrating a chalcone scaffold with a strobilurin pharmacophore. The preliminary bioassay showed that some of the chalcone analogues exhibited good in vivo fungicidal activities against Pseudoperoniospora cubensis and Sphaerotheca fuliginea at the dosage of 200 μg mL-1. Two compounds, (￡)-methyl 2-[2-({3-[(￡)-3-(2- chlorophenyl)acryloyl]phenoxy}methyl)phenyl]-3-meth-oxyacrylate (1e) and (E)-methyl 2-[2-({3-[(E)-3-(3-bromophenyl)acryloyl]phenoxy}methyl)phenyl]-3- methoxyacrylate (11), were found to display higher fungicidal activities against P. cubensis (EC90 = 118.52 μg ml-1 for 1e and EC 90 = 113.64 μg mL-1 for 11) than Kresoxim-methyl (EC90 = 154.92 μg mL-1) and were identified as the most promising candidates for further study. The present work demonstrated that strobilurin analogues containing chalcone as a side chain could be used as a lead structure for further developing novel fungicides. To our knowledge, this is the first report about the syntheses and fungicidal activities of chalcone-based strobilurin derivatives.