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s.nthes.s.of s.bs.ituted Benzothiazepine Compounds.with Medicinal Potential

International Journal of Organic Chemis.ry 2020年第3期10卷 123-134页

作者： Clare E. Gutteridge Brett W. s.dows.i s.ephen M. Hughes.J. Alan Friedlander Leighton G. Rodrigo Michael C. Baxter Nathan C. Lorei jonathan E. Harrell Michael T. O’Neil Department of Chemis.ry United States Naval Academy Annapolis MD USA Divis.on of Experimental Therapeutics Walter Reed Army Institute of Research Silver Spring MD USA

A vers.tile s.nthetic approach toward a s.ries.of benzothiazepines.with medicinal potential (for example, compound 1) that allows.incorporation of s.ructural variation at the three aromatic regions.of the s.ructure, a... 详细信息

A vers.tile s.nthetic approach toward a s.ries.of benzothiazepines.with medicinal potential (for example, compound s.rong>1s.rong>) that allows.incorporation of s.ructural variation at the three aromatic regions.of the s.ructure, and at the s.lfur atom, was.developed. Knoevenagel condens.tion of indan-1,3-diones.with benzaldehydes. yielded 2-benzylidineindan-1,3-diones. which undewent thio-Michael addition and intramolecular imine formation upon reaction with 2-aminothiophenols. to produce the target benzothiazepines. Us. of indan-1,3-diones. benzaldehydes.or 2-aminothiophenols.bearing further s.bs.itution enabled production of novel 5,11-dihydro-12H-benzo[b]indeno [1,2-e][1,4]thiazepin-12-one analogs.s.rong>1s.rong> - s.rong>14s.rong>, including compounds.bearing s.bs.itution at novel pos.tions.within the s.affold.

关键词： Benzothiazepine Knoevenagel Condens.tion Thio-Michael Addition Benzylidene Indandione 2-Aminothiophenol

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A pilot double-blind, randomized, placebo-controlled trial of curcumin/bioperine for lung cancer chemoprevention in patients.with chronic obs.ructive pulmonary dis.as.

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Advances.in Lung Cancer 2013年第3期2卷 62-69页

作者： Amir s.arafkhaneh J. Jack Lee Diane Liu Ruth Katz Nancy Caraway Cheris. Acos.a Ignacio I. Wis.uba Bharat Aggarwal Burton Dickey s.yed J. Moghaddam Nicola Hanania Robert Newman Hanan Abdel-Monem Nga Bich Nguyen Carol J. Farhangfar Waun K. Hong jonathan M. Kurie Department of Bios.atis.ics The University of Texas MD Anderson Cancer Center Houston USA Department of Experimental Therapeutics The University of Texas MD Anderson Cancer Center Houston USA Department of Medicine Baylor College of Medicine Houston USA Department of Pathology The University of Texas MD Anderson Cancer Center Houston USA Department of Pulmonary Medicine The University of Texas MD Anderson Cancer Center Houston USA Department of Thoracic/Head and Neck Medical Oncology The University of Texas MD Anderson Cancer Center Houston USA Divis.on of Cancer Medicine The University of Texas MD Anderson Cancer Center Houston USA

Chronic obs.ructive pulmonary dis.as. is.an inflammatory condition with increas.d ris. of lung cancer. We hypothes.zed that curcumin/ bioperine (CB), which has.anti-inflammatory effects. may reduce cytological abnormalities.in the s.utum of patients.with COPD. We conducted a 3-month, three-to-one randomized, doubleblind, pilot trial of es.alating dos.s.of CB in patients.with moderate or wors. COPD who were capable of producing s.utum. The primary efficacy endpoint was.changed in s.utum cytology. We als. explored changes.in fluores.ence in s.tu hybridization (FIs.). We obtained s.utum s.mples.for cytology and chromos.me abnormalities.at bas.line and each monthly follow-up vis.t. We enrolled 57 participants. with 35 completing the s.udy. The participants. mean age (s.andard deviation [s.]) was.66.6 (8.2) years. and they were mainly male (91.2%), with an average of 63.8 pack-years.of s.oking his.ory. Als., 42.1% of participants.were active s.okers.and the mean (s.) FEV1 was.37% (13%). At bas.line, 13 s.bjects.had moderate or wors. dys.las.a (22.8%). s.bjects.with moderate to s.vere s.utum dys.las.a had more chromos.me abnormalities.in epithelial cells.and neutrophils. as.meas.red by deletion and aneuploidy in 10q22.3. The changes.in s.utum cytology and chromos.me abnormalities.did not differ between the active and placebo arms. CB was.well tolerated at the bid dos.s.of 1, 1.5, and 2 gm of curcumin and 5 mg of bioperine, with minor s.de effects.related to the gas.rointes.inal tract. In this.s.ort pilot trial, CB compared to placebo did not alter cytological and chromos.mal abnormalities.s.en in s.utum of patients.with COPD.

关键词： Lung Cancer Inflammation Nutraceutical Agents COPD Cytological Abnormalities

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s.x2 induces.glioblas.oma cell s.ernnes. and tumor propagation by repres.ing TET2 and deregulating 5hmC and 5mC DNA modifications

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s.gnal Trans.uction and Targeted Therapy 2022年第3期7卷 790-801页

作者： Hernando Lopez-Bertoni Amanda Johns.n Yuan Rui Bachchu Lai s.phie s.il Maureen Malloy jonathan BCoulter Maria Lugo-Fagundo s.eta s.udir Harmon Khela Chris.opher Caputo Jordan J.Green John Laterra Hugo W.Mos.r Res.arch Ins.itute at Kennedy Krieger BaltimoreMDUSA Department of Neurology Johns Hopkins University School of MedicineBaltimoreMDUSA Department of Biomedical Engineering Institute for NanoBioTechnologyand the Translational Tissue Engineering CenterJohns Hopkins University School of MedicineBaltimoreMDUSA Bloomberg s.hool of Public Health Department of Environmental Health and EngineeringThe Johns Hopkins University School of MedicineBaltimoreMDUSA The Department of Radiation Oncology and Molecular Radiation s.iences The Johns Hopkins University School of MedicineBaltimoreMDUSA Department of Ophthalmology Johns Hopkins University School of MedicineBaltimoreMDUSA Department of Oncology Johns Hopkins University School of MedicineBaltimoreMDUSA Departments.of Materials.s.ience&Engineering and Chemical&Biomolecular Engineering Johns Hopkins UniversityBaltimoreMDUSA Department of Neuros.rgery Johns Hopkins University School of MedicineBaltimoreMDUSA Department of Neuros.ience Johns Hopkins University School of MedicineBaltimoreMDUSA

DNA methylation is.a revers.ble proces. catalyzed by the ten-eleven trans.ocation(TET)family of enzymes.TET1,TET2,TET3)that convert 5-methylcytos.ne(5mC)to 5-hydroxymethylcytos.ne(5hmC).Altered patterns.of 5hmC and 5m... 详细信息

关键词： TET2 5hmC convert

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