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有机合成创新—产业化的新动力——中国化学会全国第三届有机合成化学与过程学术讨论会

作者： Zhang,Feifei Yan,Jianping Zhou,Chenghe~* (Laboratory of Bioorganic & Medicinal Chemistry,School of Chemistry and Chemical Engineering, Southwest University,Chongqing 400715)

Carbazole and its derivatives are an important type of nitrogen-containing aromatic heterocyclic compounds, possess desirable electronic and charge-transport properties,as well as largeπ-conjugated system,and the various functional groups are easily introduced into the structurally rigid carbazolyl *** carbazole ring is present in a variety of naturally occurring medicinally active *** synthetic and natural carbazole derivatives have recently been found to exhibit a broad range of biological activity,such as antitumor,

关键词： carbazole synthesis nitroimidazole antibacterial antifungal

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Synthesis of Novel nitroimidazole Enols as Effective Anti-Pseudomonas aeruginosa Agents

Synthesis of Novel Nitroimidazole Enols as Effective Anti-Ps...

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中国化学会第十四届全国有机合成化学学术研讨会

作者： Zhen-Zhen Li Rammohan R.Yadav Bheemanaboina Cheng-He Zhou Institute of Bioorganic ＆ Medicinal Chemistry School of Chemistry and Chemical EngineeringSouthwest University

A series of novel potentially antimicrobial nitroimidazole enols 3a-i were synthesized starting from 2-methyl-5-nitroimidazole and aromatic aldehydes. Compound 3i was found to give strong anti-P. aeruginosa efficacy（MIC = 0.1 μmol/mL）, could rapidly kill P. aeruginosa strains and cleave the sensitive P. aeruginosa DNA, and be efficiently stored and carried by human serum albumin.

关键词： nitroimidazole synthesis antibacterial DNA HSA

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Design and Synthesis of Novel Amido Tetra-nitroimidazole as Potential Anticancer Agent

Design and Synthesis of Novel Amido Tetra-Nitroimidazole as ...

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有机合成创新—产业化的新动力——中国化学会全国第三届有机合成化学与过程学术讨论会

作者： Cao,Shouying Zhou,Chenghe~* (School of Chemistry and Chemical Engineering,Southwest University,Chongqing 400715)

The new millennium has witnessed considerable decrease in a number of previously fatal pathologies,largely due to the advancement in molecular medicine and modern approaches to *** spite of this success, neoplastic disease(cancer) remains a serious problem due to several reasons.A novel group of clinically interesting anticancer drugs has been a recent focus holding substantial promise as selective anticancer drugs. Imidazole compounds have been shown to suppress several types of cancer in animal models,including breast,

关键词： nitroimidazole synthesis anticancer

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Prediction of Enhancement Effect of nitroimidazoles on Irradiation by Gene Expression Programming

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Chemical Research in Chinese Universities 2013年第3期29卷 519-525页

作者： LONG Wei ZHANG Xiao-dong WANG Hao SHEN Xiu SI Hong-zong Key Laboratory of Tianjin Molecular Nuclear Medicine Institute of Radiation Medicine Peking Union Medical College Chinese Academic of Medical Sciences Tianjin 300192 P. R. China Growing Base for State Key Laboratory of New Fibrous Materials and Modern Textile Institute for Computational Science and Engineering Qingdao University Qingdao 266071 P. R. China Department of Chemistry Lanzhou University Lanzhou 730000 P. R. China

A novel machine learning method, gene expression programming（GEP）, was employed to build quatitative structure-activity relationship（QSAR） models for predicting the enhancement effect of nitroimidazole compounds on irradiation. The models were based on descriptors which were calculated from the molecular structures. Four descriptors were selected from the pool of descriptors by best multiple linear regression（BMLR） method. After that, three regression methods, multiple linear regression（MLR）, support vector machine（SVM） and GEP, were used to build QSAR models. Compared to MLR and SVM, GEP produced a better model with the square of correlation coefficient（R2）, 0.9203 and 0.9014, and the root mean square error（RMSE）, 0.6187 and 0.6875, for training set and test set, respectively. The results show that the GEP model has better predictive ability and more reliable than the MLR and SVM models. This indicates that GEP is a promising method on relevant researches in radiation area.

关键词： nitroimidazole Irradiation enhancement effect Gene expression programming

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A neutrophil-biomimic platform for eradicating metastatic breast cancer stem-like cells by redox microenvironment modulation and hypoxia-triggered differentiation therapy

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Acta Pharmaceutica Sinica B 2023年第1期13卷 298-314页

作者： Yongchao Chu Yifan Luo Boyu Su Chao Li Qin Guo Yiwen Zhang Peixin Liu Hongyi Chen Zhenhao Zhao Zheng Zhou Yu Wang Chen Jiang Tao Sun Key Laboratory of Smart Drug Delivery(Ministry of Education) Minhang HospitalState Key Laboratory of Medical Neurobiology and MOE Frontiers Center for Brain ScienceDepartment of PharmaceuticsSchool of PharmacyResearch Center on Aging and MedicineFudan UniversityShanghai 201203China

Metastasis accounts for 90%of breast cancer deaths,where the lethality could be attributed to the poor drug accumulation at the metastatic *** tolerance to chemotherapy induced by breast cancer stem cells(BCSCs)and their particular redox microenvironment further aggravate the therapeutic *** be specific,therapy-resistant BCSCs can differentiate into heterogeneous tumor cells constantly,and simultaneously dynamic maintenance of redox homeostasis promote tumor cells to retro-differentiate into stem-like state in response to cytotoxic ***,we develop a specifically-designed biomimic platform employing neutrophil membrane as shell to inherit a neutrophil-like tumor-targeting capability,and anchored chemotherapeutic and BCSCs-differentiating reagents with nitroimidazole(NI)to yield two hypoxia-responsive prodrugs,which could be encapsulated into a polymeric nitroimidazole *** platform can actively target the lung metastasis sites of triple negative breast cancer(TNBC),and release the escorted drugs upon being triggered by the hypoxia *** the responsiveness,the differentiating agent could promote transferring BCSCs into non-BCSCs,and simultaneously the nitroimidazole moieties conjugated on the polymer and prodrugs could modulate the tumor microenvironment by depleting nicotinamide adenine dinucleotide phosphate hydrogen(NADPH)and amplifying intracellular oxidative stress to prevent tumor cells retro-differentiation into *** combination,the BCSCs differentiation and tumor microenvironment modulation synergistically could enhance the chemotherapeutic cytotoxicity,and remarkably suppress tumor growth and lung ***,this work can provide a new insight in to comprehensively treat TNBC and lung metastasis using a versatile platform.

关键词： Metastasis Breast cancer Neutrophil Hypoxia Cancer stem cell Glutathione Reactive oxygen species nitroimidazole

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Novel potentially antimicrobial nitroimidazoles by exerting biosupramolecular interactions

Novel potentially antimicrobial nitroimidazoles by exerting ...

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全国第十九届大环化学暨第十一届超分子化学学术讨论会

作者：李珍珍 Rammohan R.Yadav Bheemanaboina Vijai Kumar Reddy Tangadanchu 周成合 Institute of Bioorganic&Medicinal Chemistry Key Laboratory of Applied Chemistry of Chongqing MunicipalitySchool of Chemistry and Chemical Engineering Southwest University CSIR-Indian Institute of Integrative Medicine (IIIM) Indian Institute of Chemical Technology

＜正＞A series of novel potentially antimicrobial nitroimidazoles were *** 4i was found to give stronger *** efficacy, could rapidly kill *** strains and effectively cleave the sensitive *** *** active molecule 4i could also be efficiently stored and carried by human serum albumin via supramolecular *** hydrogen bonds drive to stabilize the compound 4i-topoisomerase Ⅱ supramolecular complex.

关键词： nitroimidazole Supermolecular Antimicrobial HSA

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Synthesis and Their Supramolecular Transportation and Activity of Antimicrobial Quinazolinone nitroimidazoles

Synthesis and Their Supramolecular Transportation and Activi...

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全国第十七届大环化学暨第九届超分子化学学术研讨会

作者：彭丽萍周成合 School of Chemistry and Chemical Engineering Southwest University

＜正＞Quinolones are one of the most widely prescribed antimicrobial agents as they are generally well tolerated with excellent safety profile and favorable pharmacokinctic ***,with the increasing emergencies of micro... 详细信息

关键词： Quinazolinone nitroimidazole Antimicrobial Supramolecular Transportation

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Design and Synthesis of Novel Enone-bridged Indole nitroimidazoles and Their Supramolecular Interactions with Sensitive Bacterial DNA and HSA

Design and Synthesis of Novel Enone-bridged Indole Nitroimid...

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中国化学会·第十五届全国有机合成化学学术研讨会

作者： Zhen-Zhen Li Rammohan R.Yadav Bheemanaboina 周成合 Institute of Bioorganic & Medicinal Chemistry School of Chemistry and Chemical EngineeringSouthwest University Indian Institute of Integrative Medicine 西南大学

A series of novel enone-bridged indole nitroimidazoles were designed and *** the compounds were prepared in high yields from *** of the new compounds displayed preferable antibacterial efficacies towards the tested *** active molecule could also be efficiently stored and carried by human serum albumin and targeting sensitive bacterial DNA via supramolecular interactions.

关键词： nitroimidazole antibacterial DNA HSA

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