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Use of Silicon Substituents in the Syntheses of Natural and Non-natural Molecules

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Chinese Journal of Chemistry 2005年第8期23卷 1106-1108页

作者： WONG, Henry N. C. department of Chemistry Institute of Chinese Medicine and Central Laboratory of Institute of Molecular Technology for Drug Discovery and Synthesis The Chinese University of Hong Kong Shatin New TerritoriesHong Kong SAR China

Trimethylsilyl groups have been used in our research as a director as well as a bulky and lipophilic group in our quest for natural and non-natural molecules.

关键词： trimethylsilyl bulky group lipophilic group

Synthesis and antimycobacterial screening of new N-(4-(5-aryl-3-(5-methyl-1,3,4-oxadiazol-2-yl)-1H-pyrazol-1-yl)phenyl)-4-amide derivatives

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Chinese Chemical Letters 2016年第3期27卷 365-369页

作者： Nagabhushana Nayak Jurupula Ramprasad Udayakumar Dalimba Perumal Yogeeswari Dharmarajan Sriram Organic Chemistry Laboratory Department of ChemistryNational Institute of Technology Karnataka Medicinal Chemistry and drug discovery Research Laboratory Pharmacy GroupBirla Institute of Technology and Science-PilaniHyderabad Campus

This article demonstrates the synthesis, characterization and the study of in vitro antitubercular activities of twenty four new N-（4-（5-aryl-3-（5-methyl-1,3,4-oxadiazol-2-yl）-1H-pyrazol-1-yl）phenyl）-4-amide derivatives（8a–x）. The antitubercular activity of the compounds against Mycobacterium tuberculosis H37Rv（MTB） revealed that 2-chloro-N-（4-（5-（4-chlorophenyl）-3-（5-methyl-1,3,4-oxadiazol-2-yl）-1H-pyrazol-1-yl）phenyl）benzamide（8n） is the most promising lead molecule with a MIC of1.56 mg/m L, while the corresponding unsubstituted benzamide derivative（8o） is the next most active molecule with a MIC of 3.13 mg/m L. Interestingly, the pyrazole intermediate 5b containing chlorophenyl and N-acylcarbohydrazide substituents also showed significant activity（MIC = 3.13 mg/m L）. Further, the active molecules did not show toxicity against a normal NIH 3T3 cell line, signifying their suitability for further drug development.

关键词： Pyrazole-oxadiazole hybrids Antitubercular activity SC-XRD analysis In vitro cytotoxicity

Crystal structure determination of a chimeric FabF by XRD

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Nuclear Science and Techniques 2017年第9期28卷 63-68页

作者： Ke Li Li Li Ye-Chun Xu College of Science Shanghai University CAS Key Laboratory of Receptor Research Drug Discovery and Design Center Shanghai Institute of Materia MedicaChinese Academy of Sciences (CAS)

Beta-ketoacyl-acyl-carrier-protein synthase Ⅱ,an important enzyme in biosynthesis of bacterial fatty acid,is an attractive target in antibacterial drug design. Platensimycin(PTM), produced by Streptomyces platensis, has a strong, broad-spectrum Gram-positive antibacterial activity by selectively targeting to Fab F but exhibits no inhibition to the Fab F from Streptomyces platensis(spFabF). To study the self-resistance mechanism within the PTM-producing strain and provide hint for development of novel antibiotics, it is imperative to solve the structure of spFabF and elucidate the difference between spFabF and other Fab Fs which are not resistant to PTM. To this end, we constructed four chimeric Fab Fs based on the sequence of spFabF and its homologous protein after the expression of wide-type spFabF was failed. The crystal structure of one chimera, js_(200)FabF, of 91.2% sequence identity to spFabF,was solved. A structure comparison of js_(200)FabF with a PTM-bound Fab F suggested that three loops nearby the catalytic site might play key roles in preventing the binding of PTM to spFabF. The results provide an encouraging basis for further studies on the self-resistance mechanismand structure-based design of novel antibiotics targeting FabFs.

关键词：晶体结构嵌合体 XRD 广谱抗菌活性测定药物设计生产菌株 PTM

Recent advances in non-toxic quantum dots and their biomedical applications

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Progress in Natural Science:Materials International 2019年第6期29卷 628-640页

作者： Chunyan Zhu Zhao Chen Shuai Gao Ban Leng Goh Ismail Bin Samsudin Kai Wen Lwe Yunlong Wu Caisheng Wu Xiaodi Su Fujian Provincial Key Laboratory of Innovative drug target Research and State Key Laboratory of Cellular Stress Biology School of Pharmaceutical Sciences Xiamen University department of Chemistry National University of Singapore Institute of Materials Research and Engineering Agency for Science Technology and Research

Quantum dots(QDs) with unique quantum confinement effect and electro-optical properties are attractive for biomedical applications. Toxic effects of traditional semiconductor QDs made of heavy metal ions have serious safety concerns for their undesired environmental or healthy impact. Recent reports on core-shell structure modification of QDs by using biocompatible ligands or polymers is one way to be effectively minimizing toxicity effects of traditional QDs. Furthermore, designs of heave metal-free and metal-free QDs formulations are more promising alternatives, due to the non-toxic and eco-friendly nature of the starting materials. In article, we will review the recent designs of non-toxic or less toxic QDs, including carbon-based, biomolecules-based, siliconbased, and ternary I-III-VI QDs, and their biological applications(bio-imaging, drug delivery, gene therapy and immunoassay).

关键词： Quantum dots Non-toxic Bio-imaging Core-shell Metal-free

Cancer gene therapy targeting angiogenesis:An updated review

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World Journal of Gastroenterology 2006年第43期12卷 6941-6948页

作者： Ching-Chiu Liu Zan Shen Hsiang-Fu Kung Marie CM Lin Institute of MolecularTechnology for drug discovery and Synthesis Department ofChemistry The University of Hong Kong Pokfulam Hong KongChina Centre for Emerging Infectious Diseases TheChinese University of Hong Kong Shatin Hong Kong China

Since the relationship between angiogenesis and tumor growth was established by Folkman in 1971, scientists have made efforts exploring the possibilities in treating cancer by targeting angiogenesis. Inhibition of angiogenesis growth factors and administration of angiogenesis inhibitors are the basics of anti- angiogenesis therapy. Transfer of anti-angiogenesis genes has received attention recently not only because of the advancement of recombinant vectors, but also because of the localized and sustained expression of therapeutic gene product inside the tumor after gene transfer. This review provides the up-to-date information about the strategies and the vectors studied in the field of anti-angiogenesis cancer gene therapy.

关键词： Anti-angiogenesis Tumor growth Cancergene therapy

Five new terpenoids from Viburnum odoratissimum ***

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Chinese Journal of Natural Medicines 2023年第4期21卷 298-307页

作者： LI Yang JIAN Yajiao XU Fan LUO Yongxin LI Zhixuan OU Yi WEN Yan JIN Jingwei ZHANG Chuarui GAN Lishe School of Biotechnology and Health Sciences International Healthcare Innovation InstituteWuyi UniversityJiangmen 529020China Chongqing Key Laboratory of Natural Product Synthesis and drug Research School of Pharmaceutical SciencesChongqing UniversityChongqing 401331China Shandong Laboratory of Yantai drug discovery Bohai Rim Advanced Research Institute for Drug DiscoveryYantai 264117China College of Pharmaceutical Sciences Zhejiang UniversityHangzhou 310058China

Five new terpenoids,including two vibsane-type diterpenoids(1,2)and three iridoid allosides(3-5),together with eight known ones,were isolated from the leaves and twigs of Viburnum odoratissimum *** planar structures and relative configurations were determined by spectroscopic methods,especially 2D NMR *** sugar moieties of the iridoids were confirmed asβ-D-allose by GC analysis after acid hydrolysis and *** absolute configurations of neovibsanin Q(1)and dehydrovibsanol B(2)were determined by quantum chemical calculation of their theoretical electronic circular dichroism(ECD)spectra and Rh2(OCOCF_(3))_(4)-induced ECD *** anti-inflammatory activities of compounds 1,3,4,and 5 were evaluated using an LPS-induced RA W264.7 cell *** 3 suppressed the release of NO in a dose-dependent manner,with an IC_(50) value of 55.64μmol·L^(-1).The cytotoxicities of compounds 1-5 on HCT-116 cells were assessed and the results showed that compounds 2 and 3 exhibited moderate inhibitory activities with IC_(50) values of 13.8 and 12.3μmol·L^(-1),respectively.

关键词： Viburnum odoratissimum var.sessilifolrum Terpenoids Acid hydrolysis ECD calculation Anti-inflammation

Synthesis and Antitumor Activities of Novel 4-Morpholinothieno [3,2-d]pyrimidine Derivatives

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Chemical Research in Chinese Universities 2014年第1期30卷 75-81页

作者： SONG Kaizhen MA Junjie WANG Xiao GONG Ping ZHAO Yanfang Key Laboratory of Structure-based drug Design and discovery Ministry of Education Shenyang Pharmaceutical University Shenyang 110016 P. R. China

A series of novel 2-hydrazinyl-4-morpholinothieno[3,2-d]pyrimidine derivatives was designed and *** of them were screened for their cytotoxic activities against large cell lung cancer（H460）,colon cancer （HT-29） and adenocarcinomic lung cancer（A549） cell lines in *** pharmacological results indicate that most of the target compounds show moderate to significant *** compound 17 exhibits the most potent antitumor activities against H460,HT-29 and A549 cell lines with IC50 values of 0.57,0.45 and 1.45 μmol/L,respectively.

关键词： 2-Hydrazinyl-4-morpholinothieno[3,2-d]pyrimidine Antitumor activity Cytotoxic activity

Psychosis symptoms following aberrant immunity in the brain

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Neural Regeneration Research 2021年第3期16卷 512-513页

作者： Akitoshi Ozaki Yuki Yamawaki Gen Ohtsuki department of Biophysics Kyoto University Graduate School of ScienceKyotoJapan The Hakubi Center for Advanced Research Kyoto UniversityKyotoJapan department of drug discovery Medicine Kyoto University Graduate School of MedicineKyotoJapan

Neuroinflammation in the brain is thought related to the emergence of various psychoses,although the identifying regional significance,the involvement of immune-cells and lymphocytic activity,and ways for the therapeutic recovery are under the effort of *** recently revealed that the cerebellar acute inflammation causes the symptoms manifested in mood disorders or developmental disorders,which were associated with hyperexcitability due to immune-triggered plasticity and the overconnectivity between the inflamed cerebellum and prefrontal cortex(Yamamoto et al.,2019).

关键词： inflammation immunity involvement

Protecting future antimalarials from the trap of resistance:Lessons from artemisinin-based combination therapy (ACT) failures

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Journal of Pharmaceutical Analysis 2021年第5期11卷 541-554页

作者： Nekpen Erhunse Dinkar Sahal Malaria drug discovery Research Group International Centre for Genetic Engineering and BiotechnologyNew Delhi110067India department of Biochemistry Faculty of Life SciencesUniversity of BeninBenin CityEdo-StateNigeria

Having faced increased clinical treatment failures with dihydroartemisinin-piperaquine(DHA-PPQ),Cambodia swapped the first line artemisinin-based combination therapy(ACT)from DHA-PPQ to artesunate-mefloquine given that parasites resistant to piperaquine are susceptible to ***,triple mutants have now emerged,suggesting that drug rotations may not be adequate to keep resistance at *** is,therefore,an urgent need for alternative treatment strategies to tackle resistance and prevent its spread.A proper understanding of all contributors to artemisinin resistance may help us identify novel strategies to keep artemisinins effective until new drugs become available for their *** review highlights the role of the key players in artemisinin resistance,the current strategies to deal with it and suggests ways of protecting future antimalarial drugs from bowing to resistance as their predecessors did.

关键词： Artemisinin resistance Quiescence K13 mutations Non-K13 mutations Artemisinin-based combination therapy (ACT)failure drugs in development Malaria eradication