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Chinese Journal of Chemistry 2024年第3期42卷 271-275页

作者： Yannan Zhu Haoran Jiang Yi-Ning Wang Faculty of Chemistry and Chemical Engineering Yancheng Institute of TechnologyYanchengJiangsu224051 China

A phosphine-catalyzed [4+3] annulation between dinucleophilic indole derivatives and Morita−Baylis−Hillman (MBH) carbonates was discovered by using the N1 and N4′/C4′ nucleophilicities of the indole precursors,in which indoles act as four atom synthons. This protocol provides an efficient and facile access to indole-1,2-fused 1,4-diazepinones and azepines in good to high yields in one step,which illustrates potential synthetic utilities in drug discovery.

关键词： Phosphine catalysis [4+3]Annulation indole derivatives Nitrogen heterocycles Organocatalysis

New indole derivatives from endophytic fungus Colletotruchum sp. HK-08 originated from leaves of Nerium indicum

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Chinese Herbal Medicines 2024年第2期16卷 235-238页

作者： Huiqin Chen Hao Zheng Caihong Cai Hao Wang Cuijuan Gai Zhiqiong Tan Haofu Dai Wenli Mei Hainan Key Laboratory of Research and Development of Natural Product from Li Folk Medicine Institute of Tropical Bioscience and BiotechnologyChinese Academy of Tropical Agricultural SciencesHaikou 571101China Hainan Institute for Tropical Agricultural Resources Haikou 571101China School of Life and Pharmaceutical Sciences Hainan UniversityHaikou 570228China

Objective: To study secondary metabolites from endophytic fungus Colletotruchum sp. HK-08 originated from the leaves of Nerium indicum.Methods: The compounds were isolated by various column chromatographic techniques, and their structures were elucidated by spectroscopic techniques [high resolution electrospray ionization mass spectroscopy(HRESIMS), one-dimensional(1D) and two-dimensional(2D) nuclear magnetic resonance spectroscopy(NMR)], as well as comparison with literature data. The Ellman method was used to determine the acetylcholinesterase(ACh E) inhibitory activity.Results: Four indole derivatives were identified from Colletotruchum sp. HK-08, including 6’-hydroxymonaspiloindole(1), 2-(2-oxoindolin-3-yl)ethyl 2-(4-hydroxyphenyl) acetate(2), 2-(2-oxoindolin-3-yl)ethyl 2-(2-hydroxyphenyl)acetate(3), and monaspiloindole(4). Compound 4 presented weak ACh E inhibitory activity with IC50value of(69.30 ± 6.27) μmol/L [tacrine as the positive control, with IC50value of(0.61 ± 0.07) μmol/L].Conclusion: Compounds 1–3 were new compounds, and compound 4 had weak ACh E inhibitory activity.

关键词： Colletotruchum sp. endophytic fungus indole derivatives Nerium indicum Mill. secondary metabolites

Correlation between Chromatograph Capacity Factors and Structural Parameters of indole derivatives

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Chinese Journal of Structural Chemistry 2005年第12期24卷 1381-1386页

作者： ZHENG Qing WANG Zun-Yao SUN Li YU Bin Department of Chemical Engineering Yancheng Institute of Technolog3 Yancheng Jiangsu 224003 China School of Biological and Chemical Engineering Jiaxing University Jiaxing Zhejiang 314001 China School of Sciences Nanjing University of Technolog） Nanjing Jiangsu 210009 China

Sixteen indole derivatives have been computed at B3LYP/6-31 IG^＊＊ level using density functional theory （DFF）. Based on linear solvation energy theory, the structural parameters were employed to present correlation between the parameters of chromatograph capacity factor （CCF） and molecular structural parameters. As a result, the correlation equation of the reversed phased high performance liquid chromatograph capacity factor to the intercept lgk＇w and slope S of CCF were obtained, from which the correlation coefficients of lgk＇w to the structural parameters are r^2 = 0.9596 and q^2 = 0.9262. While the correlation coefficients of the parameter S r^2 q^2 with structures are = 0.9750 and = 0.9252. Moreover, the effect of water as solvent on the present two models was also considered using SCRF method, and the result shows that the predicting capacity of correlation equation of lgkw＇ increases, while that of the model for S decreases slightly. Both two correlation equations achieved in this work are more advantageous than those using theoretical descriptors from molecular connectivity indices.

关键词： indole derivatives quantitative structure-retention relationship （QSRR）,chromatograph capacity factor （CCF） reversed phased high performance liquid chroma-tograph （RP-HPLC） density functional theory （DFT） self-consistent reaction field（SCRF）

Low-Frequency Vibrations of indole derivatives by Terahertz Time-Domain Spectroscopy

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Journal of Electronic Science and Technology 2016年第4期14卷 329-336页

作者： Ya-Ru Dang Shao-Ping Li Hui Liu Shao-Xian Li Jian-Bing Zhang Hong-Wei Zhao School of Chemical Engineering East China University of Science and TechnologyShanghai200237China School of Precision Instrument and Optoelectronics Engineering Tianjin UniversityTianjin 300072China Key Laboratory of Interfacial Physics and Technology Shanghai Institute of Applied PhysicsChinese Academy of SciencesShanghai 201800China

Several indole derivatives with different ＇3-＇ substituents have been investigated by terahertz （THz） time-domain spectroscopy. The low-frequency absorption spectra and refractive indices were obtained in the range of 0.2 THz to 2.5 THz （7 cm-1 to 83 cm-1）. These derivatives with different substituents present distinct features, which suggests that THz spectroscopy is sensitive to different structures and components of these chemicals. The density functional theory was employed to calculate the low-frequency vibrational properties of indole-3-carboxylic acid and indole-3-propionic acid based on their crystal structures, and the intermolecular interactions were involved. Meanwhile, the temperature dependence of the spectra agreed with the calculated results. The quantitative analysis of a ternary mixture was studied by taking the THz fingerprints into account, and the results demonstrate THz spectroscopy has great potential for the practical applications in biochemistry and pharmaceutics.

关键词： Characteristic spectrum density functional theory indole derivatives low-frequency vibration terahertz.

An Efficient Preparation of 2, 3-Disubstituted indole derivatives Induced by Low-valent Titanium

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Chinese Chemical Letters 2004年第5期15卷 518-520页

作者： XueSenFAN XinYingZHANG YongMinZHANG GuiRongQU SchoolofChemicalandEnvironmentalSciences KeyLaboratoryofEnvironmentalScienceandEngineeringforCollegesandUniversitiesofHenanProvinceHenanNormalUniversityXinxiang453002 DepartmentofChemistry ZhejiangUniversity（CampusXixi）Hangzhou310028

An efficient synthesis of 2, 3-disubstituted indole derivatives through low-valent titanium induced reductive cyclization of acylamido carbonyl compounds is described.

关键词： indole derivatives low-valent titanium reductive cyclization process.

Design,synthesis and biological evaluation of indole derivatives as novel inhibitors targeting B-Raf kinase

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Chinese Chemical Letters 2014年第2期25卷 351-354页

作者： Zeng Wu Ming Yan Shi-He Hu Zhi-Cheng Yu Yong Zhu Ya-Dong Cheng Hai-Chun Liu Yan-Min Zhang Si-Hui Yao Wei-Fang Tang Tao Lu Department of Organic Chemistry China Pharmaceutical University National Nanjing Center for Drug Screening China Pharmaceutical University Laboratory of Molecular Design and Drug Discovery School of SciencesChina Pharmaceutical University State Key laboratory of Natural Medicines China Pharmaceutical University The Headmaster's Office China Pharmaceutical University

A series of novel indole derivatives were designed and synthesized and their inhibitory activity against B-Raf and HepG2 cell were also described. Among them, compounds 7a and 7b exhibited excellent potency, which sho... 详细信息

关键词： B-Raf kinase inhibitors Receptor-based drug discovery indole derivatives Biological evaluation

Discovery of novel urea-indole derivatives as reversal agents against ABCG2-mediated drug resistance

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Discovery of novel urea-indole derivatives as reversal agent...

SF3B1 modulators affect key genes in metastasis and drug influx: a new approach to fight pancreatic cancer chemoresistance

第十一届全国化学生物学学术会议

作者： Gao-Jie Ye Chao-Yun Cai Yu-qi Yang Zhe-Sheng Chen Zhuo-Xun Wu Bo Wang School of Chemistry Sun Yat-Sen University Department of Pharmaceutical Sciences College of Pharmacy and Health SciencesSt.John's University The Seventh Affiliated Hospital Sun Yat-Sen University

Multidrug resistance is characterized by the resistance of cancer cells to structurally unrelated anticancer drugs. Herein,we synthesized series of indole derivatives and identified urea-indole derivatives as reversal agents that reversed ABCG2-mediated multidrug resistance.These compounds significantly increased the accumulation of mitoxantrone(MX) in ABCG2-overexpressing NCI-H460/MX20 cells.Mechanistic studies revealed that reversal efficacies were not due to an alteration in the localization or expression level of ABCG2 in ABCG2-overexpressing cell lines,but stimulated the ATP hydrolysis of ABCG2 transporter.

关键词： indole derivatives ABCG2 Multidrug resistance

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Cancer Drug Resistance 2021年第4期4卷 904-922页

作者： Ornella Randazzo Stella M.Cascioferro Camilla Pecoraro Widad Ait Iddouch Amir Avan Barbara Parrino Daniela Carbone Ugo Perricone Godefridus J.Peters Patrizia Diana Elisa Giovannetti Department of Medical Oncology Cancer Center AmsterdamAmsterdam UMCVU University Medical CenterAmsterdam 1081 HVThe Netherlands Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche(STEBICEF) Universitàdegli Studi di PalermoPalermo 90133Italy Metabolic Syndrome Research Center Mashhad University of Medical SciencesMashhad 91886-17871Iran Cancer Research Center Mashhad University of Medical SciencesMashhad 91886-17871Iran Student Research Committee School of MedicineMashhad University of Medical SciencesMashhad 91886-17871Iran Drug Discovery Unit Fondazione Ri.MEDPalermo 90128Italy Department of Biochemistry Medical University of GdanskGdansk 80-210Poland Cancer Pharmacology Lab AIRC Start Up UnitFondazione Pisana per la ScienzaPisa 56124Italy.

Aim:Because mutations of splicing factor 3B subunit-1(SF3B1)have been identified in 4%of pancreatic ductal adenocarcinoma(PDAC)patients,we investigated the activity of new potential inhibitors of SF3B1 in combination with gemcitabine,one of the standard drugs,in PDAC cell lines.Methods:One imidazo[2,1-b][1,3,4]thiadiazole derivative(IS1)and three indole derivatives(IS2,IS3 and IS4),selected by virtual screening from an in-house library,were evaluated by the sulforhodamine-B and wound healing assay for their cytotoxic and antimigratory activity in the PDAC cells SUIT-2,Hs766t and Panc05.04,the latter harbouring the SF3B1 mutations.The effects on the splicing pattern of proto-oncogene recepteur d’origine nantais(RON)and the gemcitabine transporter human equilibrative nucleoside transporter-1(hENT1)were assessed by PCR,while the ability to reduce tumour volume was tested in spheroids of primary PDAC cells.Results:The potential SF3B1 modulators inhibited PDAC cell proliferation and prompted induction of cell death.All compounds showed an interesting anti-migratory ability,associated with splicing RON/ΔRON shift in SUIT-2 cells after 24 h exposure.Moreover,IS1 and IS4 potentiated the sensitivity to gemcitabine in both conventional 2D monolayer and 3D spheroid cultures,and these results might be explained by the statistically significant increase in hENT1 expression(P<0.05 vs.untreated control cells),potentially reversing PDAC chemoresistance.Conclusion:These results support further studies on new SF3B1 inhibitors and the role of RON/hENT1 modulation to develop effective drug combinations against PDAC.

关键词： Pancreatic ductal adenocarcinoma gemcitabine indole derivatives anti-proliferative activity anti-migratory activity SF3B1 RON hENT1