Jinhui Hu

Wuyi University

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CCDC 2225352: Experimental Crystal Structure Determination

The Cambridge Structural Database (2023)

Xueli Cui Jing Qu Jianfeng Yi Weiqiang Sun Jinhui Hu

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.

10.5517/ccdc.csd.cc2dpnkb

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Identification of sedative-hypnotic compounds shared by five medicinal Polyporales mushrooms using UPLC-Q-TOF-MS/MS-based untargeted metabolomics

Phytomedicine (2024)

Wei Chen Jun-Wen Yu Yu-Yi Deng Lut Yi Wong Chen Wang

Sedative/hypnotic

10.1016/j.phymed.2024.155355

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Citations (3)

Rh(iii)-catalyzed redox-neutral C–H alkenylation of benzamides with gem-difluorohomoallylic silyl ethers via β-H elimination

Chemical Communications (2023)

Xueli Cui Jing Qu Jianfeng Yi Weiqiang Sun Jinhui Hu

Fluorinated molecules are widely used in pharmaceutical and agrochemical industries. Herein we report the synthesis of 2-(3,3-difluoro-4-(silyloxy)but-1-en-1-yl)benzamides from the unprecedented rhodium(III)-catalyzed alkenylation of various benzamides with difluorohomoallylic silyl ethers. The practicability of this protocol is demonstrated by its broad substrate compatibility, good functional group tolerance, ready scalability and high regioselectivity. The oxygen in difluorohomoallylic silyl ethers makes β-H elimination feasible, which suppresses both the β-F elimination and dialkenylation of benzamides. This redox-neutral reaction proceeds efficiently via N-O bond cleavage without external oxidants and thus provides new opportunities for the synthesis of elaborate difluorinated compounds from readily available fluorinated synthons.

10.1039/d3cc00529a

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Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline–Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer’s Disease

Journal of Medicinal Chemistry (2018)

Zhiren Wang Jinhui Hu Xiaoping Yang Xing Feng Xingshu Li

A novel series of quinoline–indole derivatives were synthesized and evaluated as multitarget-directed ligands for the treatment of Alzheimer's disease (AD). Biological evaluation revealed that the derivatives had multifunctional profiles including antioxidant effects, blood–brain barrier (BBB) penetration, biometal chelation, Aβ aggregation modulation, neurotrophic and neuroprotective properties. Moreover, several representative target derivatives demonstrated hippocampal cell proliferation in living adult mice by intracerebroventricular (icv) injection or oral administration. Further drug-like property analysis demonstrated that the optimized compound, 8d (WI-1758), had liver microsomal metabolic stability, was well tolerated (>2000 mg/kg), and had a rational pharmacokinetic profile, as well as an oral bioavailability of 14.1% and a positive log BB (−0.19) to cross the BBB in vivo. Pharmacodynamics studies demonstrated that chronic oral administration of 8d·HCl substantially ameliorated the cognitive and spatial memory deficits in APP/PS1 AD mice and noticeably reduced overall cerebral β-amyloid deposits.

10.1021/acs.jmedchem.7b01417

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Citations (78)

Treatment with combined transfusion of frozen platelets and freshly frozen plasma in acute massive hemorrhage

Youwan Ye Chunhui He Chang-zheng Liao Xue-nian Yin Jinhui Hu

Fresh frozen plasma

Platelet Transfusion

Blood preservation

Source

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Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors

European Journal of Medicinal Chemistry (2021)

Cheng-Jun Wu Jia‐Qiang Wu Yunfei Hu Suyun Pu Yu-Ying Lin

HeLa

Microtubule polymerization

10.1016/j.ejmech.2021.113629

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Citations (21)

Associations between abnormal electroencephalogram microstates and childhood emotional abuse in adolescent depression.

PubMed (2023)

Jinhui Hu Dongdong Zhou Lin Zhao Lingli Ma Xinyu Peng

Childhood traumatic experiences greatly influenced the brain network activities of patients with depression, and there is an urgent need to explore the temporal dynamics for these changes. This study aims to investigate the abnormalities of resting-state electroencephalogram (EEG) microstates in eye-open state of depressed adolescents and to explore the correlations between their EEG microstates and the childhood traumatic experience.

Ministate

Depression

10.11817/j.issn.1672-7347.2023.230220

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Citations (1)

Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer’s disease

Bioorganic & Medicinal Chemistry (2018)

Jinhui Hu Baijiao An Tingting Pan Zhengcunxiao Li Ling Huang

Ebselen

IC50

Histone deacetylase inhibitor

10.1016/j.bmc.2018.10.022

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Citations (21)

Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo

Journal of Medicinal Chemistry (2016)

Jun Yan Jie Chen Shun Zhang Jinhui Hu Ling Huang

Twenty-nine novel indole-chalcone derivatives were synthesized and evaluated for antiproliferative activity. Among them, 14k exhibited most potent activity, with IC50 values of 3-9 nM against six cancer cells, which displayed a 3.8-8.7-fold increase in activity when compare with compound 2. Further investigation revealed 14k was a novel tubulin polymerization inhibitor binding to the colchicine site. Its low cytotoxicity toward normal human cells and nearly equally potent activity against drug-resistant cells revealed the possibility for cancer therapy. Cellular mechanism studies elucidated 14k arrests cell cycle at G2/M phase and induces apoptosis along with the decrease of mitochondrial membrane potential. Furthermore, good metabolic stability of 14k was observed in mouse liver microsomes. Importantly, 14k and its phosphate salt 14k-P inhibited tumor growth in xenograft models in vivo without apparent toxicity, which was better than the reference compound CA-4P and 2. In summary, 14k deserves consideration for cancer therapy.

Chalcone

10.1021/acs.jmedchem.6b00021

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Citations (150)

Electrochemically Driven para‐Selective C(sp²)−H Alkylation Enabled by Activation of Alkyl Halides without Sacrificial Anodes

Chemistry - A European Journal (2024)

Xinling Li Weijie Deng Yating Wen Ziliang Wang Jianfeng Zhou

Abstract With alkyl halides (I, Br, Cl) as a coupling partner, an electrochemically driven strategy for para ‐selective C(sp 2 )−H alkylation of electron‐deficient arenes (aryl esters, aldehydes, nitriles, and ketones) has been achieved to access diverse alkylated arenes in one step. The reaction enables the activation of alkyl halides in the absence of sacrificial anodes, achieving the formation of C(sp 2 )‐C(sp 3 ) bonds under mild electrolytic conditions. The utility of this protocol is reflected in high site selectivity, broad substrate scope, and scalable.

10.1002/chem.202400010

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Citations (2)