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9 results on '"Leichuan Xu"'

1. Synthesis and Antifungal Activity of New butenolide Containing Methoxyacrylate Scaffold

Author

Qian Zhang, Yihao Li, Bin Zhao, Leichuan Xu, Haoyun Ma, and Mingan Wang

Subjects
butenolide, methoxyacrylate, synthesis, antifungal activity, Organic chemistry, QD241-441
Abstract

In order to improve the antifungal activity of new butenolides containing oxime ether moiety, a series of new butenolide compounds containing methoxyacrylate scaffold were designed and synthesized, based on the previous reports. Their structures were characterized by 1H NMR, 13C NMR, HR-MS spectra, and X-ray diffraction analysis. The in vitro antifungal activities were evaluated by the mycelium growth rate method. The results showed that the inhibitory activities of these new compounds against Sclerotinia sclerotiorum were significantly improved, in comparison with that of the lead compound 3–8; the EC50 values of V-6 and VI-7 against S. sclerotiorum were 1.51 and 1.81 mg/L, nearly seven times that of 3–8 (EC50 10.62 mg/L). Scanning electron microscopy (SEM) and transmission electron microscopy (TEM) observation indicated that compound VI-3 had a significant impact on the structure and function of the hyphal cell of S. sclerotiorum mycelium and the positive control trifloxystrobin. Molecular simulation docking results indicated that the introduction of methoxyacrylate scaffold is beneficial to improving the antifungal activity of these compounds against S. sclerotiorum, which can be used as the lead for further structure optimization.

Published
2022
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3. Design, Synthesis, and Fungicidal Activity of Novel Plant Elicitors Based on a Diversity-Oriented Synthesis Strategy

Author

Yihao Li, Leichuan Xu, Haoyun Ma, Yanhao Su, Qian Zhang, Yu Zhao, and Mingan Wang

Subjects
Gene Expression Regulation, Plant, Oxylipins, Botrytis, Cyclopentanes, General Chemistry, Salicylic Acid, General Agricultural and Biological Sciences, Phenylalanine Ammonia-Lyase, Plant Diseases
Abstract

The novel plant elicitors, 3-benzyl-5-[1-(2-oxo-4-phenyl-1-oxaspiro[4.5]dec-3-en-3-yl)ethylidene]-2-aminoimidazolin-4-one derivatives, were designed based on the diversity-oriented synthesis strategy and synthesized in four steps via the Knoevenagel condensation reaction as the key step. They were characterized by

Published
2022

4. Total synthesis, structure revision and cytotoxic activity of Sch 53825 and its derivatives

Author

Leichuan Xu, Haoyun Ma, Xinkun An, Yihao Li, Qian Zhang, Xinlei Liu, and Mingan Wang

Subjects
General Chemical Engineering, General Chemistry
Abstract

The first total synthesis of Sch 53825 (14) was achieved in 12 steps from 5-hydroxy-1-tetralone in 16% overall yield through N-benzyl cinchoninium chloride-catalyzed asymmetric epoxidation and a Mitsunobu reaction as the key steps.

Published
2022

8. Anticancer properties of novel pyrazole-containing biguanide derivatives with activating the adenosine monophosphate-activated protein kinase signaling pathway

Author

Xiaoping Yang, Xin Hu, Wei Wang, Jun Deng, Zhiren Wang, Ting Tao, Simeng Xu, Mengru Cao, Leichuan Xu, Caimei He, Sichun Zhou, Aiying Guan, and Di Xiao

Subjects
Adenosine monophosphate, medicine.drug_class, Cell Survival, Biguanides, Pharmaceutical Science, Antineoplastic Agents, Pharmacology, Phenformin, AMP-Activated Protein Kinases, 01 natural sciences, chemistry.chemical_compound, Inhibitory Concentration 50, Cell Movement, Cell Line, Tumor, Drug Discovery, medicine, Humans, Protein kinase A, PI3K/AKT/mTOR pathway, Cell Proliferation, Molecular Structure, 010405 organic chemistry, Biguanide, Cell growth, 0104 chemical sciences, Metformin, 010404 medicinal & biomolecular chemistry, chemistry, Pyrazoles, Signal transduction, medicine.drug, Signal Transduction
Abstract

Biguanides, including metformin and phenformin, have emerged as promising anticancer agents. However, the high dose needed for their efficient anticancer properties restricts their clinical application. In an attempt to obtain higher active compounds than these parent compounds, pyrazole-containing biguanide derivatives were synthesized and screened for in vitro cytotoxicity against human cancer cell lines. Clonogenic assays and scratch wound healing assays demonstrated that these new derivatives profoundly inhibit cell proliferation and migration. Compounds 10b and 10d exhibited strong potency with low IC50 values in the range of 6.9-28.3 μM, far superior to phenformin and metformin. Moreover, 20 μM 10b and 10d resulted in 72.3-88.2% (p

Published
2019

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