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Design,synthesis and antifungal activities in vitro of novel tetralin compounds

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Chinese Chemical Letters 2008年第3期19卷 264-268页

作者： hui Tang You Jun Zhou Yao Wu Li Jia Guo Lv can hui zheng Jun Chen Ju Zhu Department of Medicinal Chemistry School of Pharmacy Second Military Medical University Shanghai 200433 China

Novel chiral tetralin compounds were designed and synthesized, and their antifungal activities in vitro were tested. The results showed that all of target compounds had potent antifungal activities, and were stronger than that of control compounds tetrahydroisoquinolines. The binding model of lead molecules in the active site of CYP51 of candida albicans showed that lead compound specifically interacted with the amino acids residues in the active site, without binding with the heme of CYP51, which was different from azole antifungal drugs. The present study might afford a novel lead molecule to develop non-azole CYP51 inhihitars of fungi.

关键词： Antifungal Chiral tetralins Lanosterol 14α-demethylase Design Synthesis

Acidic rearrangement of benzyl group in flavone benzyl ethers and its regioselectivity

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Chinese Chemical Letters 2015年第6期26卷 793-796页

作者： Chong-Qing Wang Xin Chen Jun-Hang Jiang hui Tang Kong-Kai Zhu You-Jun Zhou can-hui zheng Ju Zhu School of Pharmacy Second Military Medical University School of Biology and Pharmaceutical Engineering Wuhan Polytechnic University Pharmacy Provincial Hospital Affiliated to Shandong University State Key Laboratory of Drug Research Shanghai Institute of Materia MedicaChinese Academy of Sciences

The benzyl-substituted flavone compounds are rare in nature, while some of which have interesting biological activities. The total synthesis of benzyl-substituted flavone derivatives via the acidic rearrangement of benzyl groups in flavone benzyl ethers, and the complicated regioselectivity of the rearrangement were reported. The regioselectivity was proposed to be determined by the steric hindrance as well as the ease of electrophilic substitution reaction for benzyl cations at different positions of corresponding debenzylated fiavone compounds.

关键词： Benzyl-substituted flavone Acidic rearrangement of benzyl group Regioselectivity Quantum chemical calculation

Design, Synthesis and Biological Evaluation of Non-azole Inhibitors of Lanosterol 14α-Demethylase of Fungi

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Chinese Chemical Letters 2006年第9期17卷 1189-1192页

作者： Bin YAO You Jun ZHOU Jü ZHU Jia Guo Lü Yao Wu LI Jun CHENG Qing Feng JIANG can hui zheng School of Pharmacy Second Military Medicial University Shanghai 200433

Novel tetralin compounds were designed and synthesized on the three-dimensional model of lanosterol 14α-demethylase of candida albicans. All of the lead compounds exhibited potent antifungal activities, especially compounds 16, 20. The mode of the action of the lead compounds was different from that of azoles. The present study affords the possibility to develop novel antifungal agents that specifically interact with the amino acid residues in the active site and avoid the serious toxicity arising from coordination binding with the heme of mammalian P450s.

关键词： Antifungal 2-aminotetralins lanosterol 14α-demethylase inhibitor.

Total Synthesis of Phakellistatin 13 by Solution Method

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Chinese Chemical Letters 2006年第8期17卷 995-998页

作者： Qing Feng JIANG You Jun ZHOU Jian Zhong YAO Jia Guo LU Ju ZHU Chun Quan SHENG can hui zheng Bing YAO Department of Medicinal Chemistry School of Pharmacy Second Military Medical University Shanghai 200433

Phakellistatin 13 is a good antitumor lead compound isolated from halobios. It was synthesized first time by solution method in combination of stepwise coupling and segment condensation. Final deprotection and cyclization were achieved according to our designed method, which was different from the reported process. The spectral data of synthetic product is consisted with literatureal data of natural product. Total synthesis of phakellistatin 13 is a significant achievement to further study of its derivatives and developing novel antitumor drugs.

关键词： Phakellistatin 13 solution-phase synthesis cyclopeptide.

Synthesis and biological evaluation of 5,6,7-trimethoxy-1-benzylidene-3,4-dihydro-naphthalen-2-one as tubulin-polymerization inhibitors

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Chinese Chemical Letters 2015年第5期26卷 607-609页

作者： Jun-Hang Jiang can-hui zheng Chong-Qing Wang Juan Wang Wei Tian Chao Yang Yun-Long Song Yong Hu Ju Zhu You-Yun Zhou School of Pharmacy Second Military Medical University Shanghai Institute of Pharmaceutical Industry Department of Neonatology Shanghai Children's HospitalShanghai Jiao Tong University

A series of new combretastatin-A4 analogs were synthesized, in which a six-membered ring connects the linking bridge and A ring, and their tumor cell growth and tubulin-polymerization inhibitory activity were evaluated. These compounds appear to be potential tubulin-polymerization inhibitors, Compounds 1b with amino substituted on position 3 of B ring conferred optimal bioactivity, higher than that of the lead compound 22b and equivalent to that of CA-4. The binding modes of these compounds to tuhulin were obtained by molecular docking, which can explain the structure-activity relationship. The studies presented here provide a new structural type for the development of novel antitumor agents.

关键词： Tubulin polymerization inhibitor Antitumor agent Combretastatin-A4 analog

Adhesion property of AlCrNbSiTi high-entropy alloy coating on zirconium:experimental and theoretical studies

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Nuclear Science and Techniques 2024年第8期35卷 79-91页

作者： Bao‑Liang Zhang Wen‑Guan Liu Meng‑He Tu can Fang Yan Liu Yu‑hui Wang Yong Hu hui Wang China Institute of Atomic Energy Beijing 102413China Sino‑French Institute of Nuclear Engineering and Technology Sun Yat-Sen UniversityZhuhai 519082China School of Power and Mechanical Engineering Wuhan UniversityWuhan 430072China

Experimental scratch tests and first-principles calculations were used to investigate the adhesion property of AlCrNbSiTi high-entropy alloy(HEA)coatings on zirconium *** HEA and Cr coatings were deposited on Zr alloy substrates using multi-arc ion plating technology,and scratch tests were subsequently conducted to estimate the adhesion property of the *** results indicated that Cr coatings had better adhesion strength than HEA coatings,and the HEA coatings showed *** special quasi-random structure approach was used to build HEA models,and Cr/Zr and HEA/Zr interface models were employed to investigate the cohesion between the coatings and Zr substrate using first-principles *** calculated interface energies showed that the cohesion between the Cr coating and the Zr substrate was stronger than that of the HEA coating with *** contrary to Al or Si in the HEA coating,Cr,Nb,and Ti atoms binded strongly with Zr *** on the calculated elastic constants,it was found that low Cr and high Al content decreased the mechanical performances of HEA ***,this study demonstrated the utilization of a combined approach involving first-principles calculations and experimental studies for future HEA coating development.

关键词： High-entropy alloy coating Cr coating Adhesion property Scratch test First-principles calculation

Influence of filler characteristics on particle removal in fluid catalytic cracking slurry under an alternating electric field

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Petroleum Science 2024年第3期21卷 2102-2111页

作者： Qiang Li hui-Zhen Yang can Yang Qing-Zhu Qiu Wei-Wei Xu Zhao-Zeng Liu College of New Energy China University of Petroleum(East China)Qingdao266580ShandongChina

The characteristics of the packing material under an alternating electric field are an important factor in the removal of FCCS *** this study,the electric field distribution of a separation unit consisting of packed spheres under an alternating electric field is simulated,and the movement mechanism of catalyst particles is ***"effective contact point"model is derived to predict the adsorption of filler contact points on catalyst particles under the alternating electric field,and the model is validated by simulations and *** numerical calculation and experimental results indicate that the electrical properties of the filler spheres,the filler angleθ,and the frequency f of the alternating electric field affect the adsorption of catalyst *** the frequency of the electric field increases,the particle removal efficiency of the high-conductivity filler(silicon carbide)increases and then settles,and the separation efficiency of the low-conductivity filler(glass,zirconia)is not sensitive to the change in electric field frequency.

关键词： Fluid catalyticcracking slurry(FCCS) Particle AC electric field Fillers Removal

Mold breakout prediction based on computer vision and machine learning

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Journal of Iron and Steel Research International 2024年第8期31卷 1947-1959页

作者： Yan-yu Wang Qi-can Wang Yong-chang Zhang Yong-hui Cheng Man Yao Xu-dong Wang School of Materials Science and Engineering Dalian University of TechnologyDalian 116024LiaoningChina Key Laboratory of Solidification Control and Digital Preparation Technology Dalian University of TechnologyDalian 116024LiaoningChina

Breakout is the most serious production accident in continuous casting and must be detected and predicted by stable and reliable *** sticking region,which forms on the local copper plate and expanded into a"V"shape,is the typical precursor of ***,computer vision technology was exploited to visualize the temperature change rate of the copper plate based on the temperature signals from thermocouples;then,the static and dynamic features of the abnormal sticking region were ***,logistic regression and Adaboost models were used to study and identify these features,resulting in the development of a mold breakout prediction model based on computer vision and machine *** test results demonstrate that the proposed model can effectively distinguish anomalous temperature patterns and considerably reduce false alarms without any missing *** a result,the proposed method could offer valuable insights into the realm of abnormality detection and prediction during continuous casting process.

关键词： Abnormality detection Image processing Adaboost Logistic regression Continuous casting

Solidification behaviour and hot cracking susceptibility of a novel Ni-based superalloy

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Journal of Iron and Steel Research International 2024年第4期31卷 956-966页

作者： Yue Chen Shao-min Lv Xing-fei Xie Xiao-can Wen Jng-long Qu Jin-hui Du High-Temperature Materials Institute China Iron and Steel Research Institute Group Co.Ltd.Beijing 100081China Beijing GAONA Materials and Technology Co. Ltd.Beijing 100081China Sichuan CISRI-GAONA Forging Co. Ltd.Deyang 610000SichuanChina

A novel Ni-based superalloy GH4151,with a γ′ volume fraction of about 55%and a service temperature capability up to 8oo oC,was *** to the different cooling conditions of various regions during the solidification of ingots,significant cooling rate variations may lead to the occurrence of hot *** scanning laser microscope was utilised to investigate the solidification process and phase precipitation behaviour of the GH4151 under wide range cooling *** characteristics of L→γ transformation were analysed,and the growth rates of at each stage were *** segregation behaviour was predicted using the Scheil equation,and the predicted results match well with the experimental *** sensitivity coefficient for hot cracking was modified,and cracking sensitivity coefficient values for the alloy under different cooling rates were computed,revealing that the alloy is most susceptible to hot cracking at 10℃/min cooling ***,controlling the cooling rate can reduce the possibility of hot cracking in ingot.

关键词： Ni-based superalloy Solidification behaviour In-situ observation Clyne and Davies's criterion:Hot cracking susceptibility