Challenging the anticolorectal cancer capacity of quinoxaline-based scaffold via triazole ligation unveiled new efficient dual VEGFR-2/MAO-B inhibitors.

[1]  M. Abdelgawad,et al.  Design, Synthesis, Molecular Modeling, and Anticancer Evaluation of New VEGFR-2 Inhibitors Based on the Indolin-2-One Scaffold , 2022, Pharmaceuticals.

[2]  J. Mialet-Perez,et al.  Monoamine Oxidase Inhibitors Prevent Glucose-Dependent Energy Production, Proliferation and Migration of Bladder Carcinoma Cells , 2022, International journal of molecular sciences.

[3]  M. Carda,et al.  Synthesis and Biological Evaluation of Small Molecules as Potential Anticancer Multitarget Agents , 2022, International journal of molecular sciences.

[4]  Hao Wang,et al.  HIF1α/VEGF Feedback Loop Contributes to 5-Fluorouracil Resistance , 2022, Frontiers in Pharmacology.

[5]  B. Mroczko,et al.  Relationship between VEGF Family Members, Their Receptors and Cell Death in the Neoplastic Transformation of Colorectal Cancer , 2022, International journal of molecular sciences.

[6]  M. Ismail,et al.  Exploration of Nitroaromatic Antibiotics via Sanger’s Reagent: Synthesis, In Silico, and Antimicrobial Evaluation , 2022, ACS omega.

[7]  Serkan Levent,et al.  Novel Thiosemicarbazone Derivatives: In Vitro and In Silico Evaluation as Potential MAO-B Inhibitors , 2021, Molecules.

[8]  H. Gul,et al.  Monoamine Oxidase (MAO) as a Potential Target for Anticancer Drug Design and Development , 2021, Molecules.

[9]  H. Alkahtani,et al.  New quinoxaline-based VEGFR-2 inhibitors: design, synthesis, and antiproliferative evaluation with in silico docking, ADMET, toxicity, and DFT studies , 2021, RSC advances.

[10]  A. Al-Harrasi,et al.  Synthesis of New 1H-1,2,3-Triazole Analogs in Aqueous Medium via “Click” Chemistry: A Novel Class of Potential Carbonic Anhydrase-II Inhibitors , 2021, Frontiers in Chemistry.

[11]  S. Ilgın,et al.  Synthesis of new hydrazone derivatives and evaluation of their monoamine oxidase inhibitory activity. , 2021, Bioorganic chemistry.

[12]  A. Amer,et al.  Halting colorectal cancer metastasis via novel dual nanomolar MMP-9/MAO-A quinoxaline-based inhibitors; design, synthesis, and evaluation. , 2021, European journal of medicinal chemistry.

[13]  İ. Şahin,et al.  Synthesis, Characterization, and Antioxidant and Anticancer Activity of 1,4-Disubstituted 1,2,3-triazoles , 2021, Journal of Molecular Structure.

[14]  Z. Kaplancıklı,et al.  Novel 2,5-disubstituted-1,3,4-oxadiazole derivatives as MAO-B inhibitors: Synthesis, biological evaluation and molecular modeling studies. , 2021, Bioorganic chemistry.

[15]  X. Qian,et al.  Design, synthesis, and in vitro and in vivo anti-angiogenesis study of a novel vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitor based on 1,2,3-triazole scaffold. , 2020, European journal of medicinal chemistry.

[16]  Xiao-dong Zhu,et al.  VEGF promotes migration and invasion by regulating EMT and MMPs in nasopharyngeal carcinoma , 2020, Journal of Cancer.

[17]  Yuxin Li,et al.  Potential monoamine oxidase A inhibitor suppressing paclitaxel‐resistant non‐small cell lung cancer metastasis and growth , 2020, Thoracic cancer.

[18]  M. Hsiao,et al.  Monoamine Oxidase B Expression Correlates with a Poor Prognosis in Colorectal Cancer Patients and Is Significantly Associated with Epithelial-to-Mesenchymal Transition-Related Gene Signatures , 2020, International journal of molecular sciences.

[19]  Hany E. A. Ahmed,et al.  Design, synthesis, molecular modelling and in vitro screening of monoamine oxidase inhibitory activities of novel quinazolyl hydrazine derivatives , 2020, Royal Society Open Science.

[20]  Mamdouh M. Ali,et al.  Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors. , 2019, European journal of medicinal chemistry.

[21]  Xin Liang,et al.  Hypoxia Induces Drug Resistance in Colorectal Cancer through the HIF-1α/miR-338-5p/IL-6 Feedback Loop. , 2019, Molecular therapy : the journal of the American Society of Gene Therapy.

[22]  J. Werner,et al.  Mechanisms of Metastasis in Colorectal Cancer and Metastatic Organotropism: Hematogenous versus Peritoneal Spread , 2019, Journal of oncology.

[23]  Marwa M. Abu‐Serie,et al.  Dual VEGFR-2/PIM-1 kinase inhibition towards surmounting the resistance to antiangiogenic agents via hybrid pyridine and thienopyridine-based scaffolds: Design, synthesis and biological evaluation. , 2019, Bioorganic chemistry.

[24]  Mohamed A. Zeidan,et al.  Design, synthesis and docking study of novel picolinamide derivatives as anticancer agents and VEGFR-2 inhibitors. , 2019, European journal of medicinal chemistry.

[25]  C. Popoiu,et al.  Monoamine Oxidase-Related Vascular Oxidative Stress in Diseases Associated with Inflammatory Burden , 2019, Oxidative medicine and cellular longevity.

[26]  S. Ilgın,et al.  In vitro and in silico evaluation of new thiazole compounds as monoamine oxidase inhibitors. , 2019, Bioorganic chemistry.

[27]  H. Fahmy,et al.  Design, synthesis and pharmacological evaluation of some substituted dihydropyrimidines with L-/T-type calcium channel blocking activities. , 2019, Bioorganic chemistry.

[28]  Marawan Ahmed,et al.  Design, synthesis, biological evaluation and dynamics simulation of indazole derivatives with antiangiogenic and antiproliferative anticancer activity. , 2019, Bioorganic chemistry.

[29]  Qi Wang,et al.  HIF‐1α/VEGF signaling‐mediated epithelial–mesenchymal transition and angiogenesis is critically involved in anti‐metastasis effect of luteolin in melanoma cells , 2019, Phytotherapy research : PTR.

[30]  Prashanth Rawla,et al.  Epidemiology of colorectal cancer: incidence, mortality, survival, and risk factors , 2019, Przeglad gastroenterologiczny.

[31]  Kiyohito Tanaka,et al.  GRIM‐19 repressed hypoxia‐induced invasion and EMT of colorectal cancer by repressing autophagy through inactivation of STAT3/HIF‐1α signaling axis , 2018, Journal of cellular physiology.

[32]  H. Stark,et al.  Selenazolyl-hydrazones as Novel Selective MAO Inhibitors With Antiproliferative and Antioxidant Activities: Experimental and In-silico Studies , 2018, Front. Chem..

[33]  Andreas Eckert,et al.  ProTox-II: a webserver for the prediction of toxicity of chemicals , 2018, Nucleic Acids Res..

[34]  E. Uriarte,et al.  Tight-Binding Inhibition of Human Monoamine Oxidase B by Chromone Analogs: A Kinetic, Crystallographic, and Biological Analysis. , 2018, Journal of medicinal chemistry.

[35]  S. Hill,et al.  Molecular Pharmacology of VEGF-A Isoforms: Binding and Signalling at VEGFR2 , 2018, International journal of molecular sciences.

[36]  A. Tripathi,et al.  Privileged scaffolds as MAO inhibitors: Retrospect and prospects. , 2018, European journal of medicinal chemistry.

[37]  D. Mochly‐Rosen,et al.  Monoamine oxidase-dependent endoplasmic reticulum-mitochondria dysfunction and mast cell degranulation lead to adverse cardiac remodeling in diabetes , 2018, Cell Death & Differentiation.

[38]  B. Korkut,et al.  Design, synthesis and biological assessment of new thiazolylhydrazine derivatives as selective and reversible hMAO-A inhibitors. , 2018, European journal of medicinal chemistry.

[39]  Daeui Park,et al.  Potent inhibitions of monoamine oxidase A and B by acacetin and its 7-O-(6-O-malonylglucoside) derivative from Agastache rugosa. , 2017, International journal of biological macromolecules.

[40]  Mamdouh M. Ali,et al.  Design, synthesis, molecular docking and cytotoxic evaluation of novel 2-furybenzimidazoles as VEGFR-2 inhibitors. , 2017, European journal of medicinal chemistry.

[41]  S. Ilgın,et al.  Synthesis of New Hydrazone Derivatives for MAO Enzymes Inhibitory Activity , 2017, Molecules.

[42]  L. Ellis,et al.  Intracrine VEGF signalling mediates colorectal cancer cell migration and invasion , 2017, British Journal of Cancer.

[43]  S. Ilgın,et al.  MAO enzymes inhibitory activity of new benzimidazole derivatives including hydrazone and propargyl side chains. , 2017, European journal of medicinal chemistry.

[44]  F. J. Luque,et al.  Design, synthesis and biological evaluation of N-methyl-N-[(1,2,3-triazol-4-yl)alkyl]propargylamines as novel monoamine oxidase B inhibitors. , 2016, Bioorganic & medicinal chemistry.

[45]  S. Jun,et al.  Inhibitory effect of traditional oriental medicine-derived monoamine oxidase B inhibitor on radioresistance of non-small cell lung cancer , 2016, Scientific Reports.

[46]  D. Baskin,et al.  Monoamine oxidase B levels are highly expressed in human gliomas and are correlated with the expression of HiF-1α and with transcription factors Sp1 and Sp3 , 2015, Oncotarget.

[47]  Rui M. V. Abreu,et al.  Synthesis, antiangiogenesis evaluation and molecular docking studies of 1-aryl-3-[(thieno[3,2-b]pyridin-7-ylthio)phenyl]ureas: Discovery of a new substitution pattern for type II VEGFR-2 Tyr kinase inhibitors. , 2015, Bioorganic & medicinal chemistry.

[48]  Sherine N. Khattab,et al.  Exploring new selective 3-benzylquinoxaline-based MAO-A inhibitors: design, synthesis, biological evaluation and docking studies. , 2015, European journal of medicinal chemistry.

[49]  Nasser S. M. Ismail,et al.  Design, synthesis and biological evaluation of type-II VEGFR-2 inhibitors based on quinoxaline scaffold. , 2014, Bioorganic chemistry.

[50]  M. Abdelgawad,et al.  Design, synthesis and cytotoxic activity of some novel compounds containing pyrazolo[3,4-d]pyrimidines nucleus , 2013, Journal of Chemical Sciences.

[51]  Raj Kumar,et al.  Lipophilicity Indices for Drug Development , 2013 .

[52]  Jianping Chen,et al.  Dietary Compound Isoliquiritigenin Inhibits Breast Cancer Neoangiogenesis via VEGF/VEGFR-2 Signaling Pathway , 2013, PloS one.

[53]  Patrick Barton,et al.  In silico physicochemical parameter predictions. , 2013, Molecular pharmaceutics.

[54]  B. Bao,et al.  The biological kinship of hypoxia with CSC and EMT and their relationship with deregulated expression of miRNAs and tumor aggressiveness. , 2012, Biochimica et biophysica acta.

[55]  M. McTigue,et al.  Molecular conformations, interactions, and properties associated with drug efficiency and clinical performance among VEGFR TK inhibitors , 2012, Proceedings of the National Academy of Sciences.

[56]  Xiao‐Yu Yin,et al.  Monoamine oxidase A expression is suppressed in human cholangiocarcinoma via coordinated epigenetic and IL-6-driven events , 2012, Laboratory Investigation.

[57]  G. Ecker,et al.  Structure–Activity Relationships, Ligand Efficiency, and Lipophilic Efficiency Profiles of Benzophenone-Type Inhibitors of the Multidrug Transporter P-Glycoprotein , 2012, Journal of medicinal chemistry.

[58]  A. Mattevi,et al.  The ‘gating’ residues Ile199 and Tyr326 in human monoamine oxidase B function in substrate and inhibitor recognition , 2011, The FEBS journal.

[59]  V. Pore,et al.  Click chemistry: 1,2,3-triazoles as pharmacophores. , 2011, Chemistry, an Asian journal.

[60]  Sherine N. Khattab,et al.  A regio- and stereo-controlled approach to triazoloquinoxalinyl C-nucleosides. , 2010, Carbohydrate Research.

[61]  Qing Zhu,et al.  'Click' assembly of selective inhibitors for MAO-A. , 2010, Bioorganic & medicinal chemistry letters.

[62]  Sherine N. Khattab,et al.  Synthesis of new series of quinoxaline based MAO-inhibitors and docking studies. , 2010, European journal of medicinal chemistry.

[63]  H. Ban,et al.  Suppression of hypoxia-induced HIF-1alpha accumulation by VEGFR inhibitors: Different profiles of AAL993 versus SU5416 and KRN633. , 2010, Cancer letters.

[64]  Christopher Hulme,et al.  The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors: a structural analysis of the binding interactions of Gleevec, Nexavar, and BIRB-796. , 2010, Bioorganic & medicinal chemistry.

[65]  Hongyang Wang,et al.  Suppression of cyclin D1 by hypoxia-inducible factor-1 via direct mechanism inhibits the proliferation and 5-fluorouracil-induced apoptosis of A549 cells. , 2010, Cancer research.

[66]  Dan Cao,et al.  Expression of HIF-1alpha and VEGF in colorectal cancer: association with clinical outcomes and prognostic implications , 2009, BMC Cancer.

[67]  K. Murakami,et al.  A graphical method for determining inhibition constants , 2009, Journal of enzyme inhibition and medicinal chemistry.

[68]  Bo Wang,et al.  New insights into the structural characteristics and functional relevance of the human cytochrome P450 2D6 enzyme , 2009, Drug metabolism reviews.

[69]  György M. Keserü,et al.  The influence of lead discovery strategies on the properties of drug candidates , 2009, Nature Reviews Drug Discovery.

[70]  Marc Coram,et al.  The significance of monoamine oxidase-A expression in high grade prostate cancer. , 2008, The Journal of urology.

[71]  Y. Collan,et al.  VEGF-1 expression in colorectal cancer is associated with disease localization, stage, and long-term disease-specific survival. , 2008, Anticancer research.

[72]  S. Bembenek,et al.  Ligand binding efficiency: trends, physical basis, and implications. , 2008, Journal of medicinal chemistry.

[73]  Sherine N. Khattab,et al.  Synthesis of 3-benzyl-2-substituted quinoxalines as novel monoamine oxidase A inhibitors. , 2006, Bioorganic & medicinal chemistry letters.

[74]  Xiaolin Ma,et al.  Predictive model of blood-brain barrier penetration of organic compounds , 2005, Acta Pharmacologica Sinica.

[75]  A. Mercurio,et al.  The epithelial-mesenchymal tansition (EMT) and colorectal cancer progression , 2005, Cancer biology & therapy.

[76]  C. Pargellis,et al.  Thermal denaturation: a method to rank slow binding, high-affinity P38alpha MAP kinase inhibitors. , 2003, Journal of medicinal chemistry.

[77]  W. Föllmann,et al.  Primary cell cultures of bovine colon epithelium: isolation and cell culture of colonocytes. , 2000, Toxicology in vitro : an international journal published in association with BIBRA.

[78]  M. Kataoka,et al.  Optimized conditions for prediction of intestinal drug permeability using Caco-2 cells. , 2000, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[79]  P. Furet,et al.  Strategies toward the design of novel and selective protein tyrosine kinase inhibitors. , 1999, Pharmacology & therapeutics.

[80]  M. Yazdanian,et al.  Correlating Partitioning and Caco-2 Cell Permeability of Structurally Diverse Small Molecular Weight Compounds , 1998, Pharmaceutical Research.

[81]  Shiyin Yee,et al.  In Vitro Permeability Across Caco-2 Cells (Colonic) Can Predict In Vivo (Small Intestinal) Absorption in Man—Fact or Myth , 1997, Pharmaceutical Research.

[82]  E. LaVoie,et al.  Bioisosterism: A Rational Approach in Drug Design. , 1996, Chemical reviews.

[83]  T. Mosmann.  Rapid colorimetric assay for cellular growth and survival: application to proliferation and cytotoxicity assays. , 1983, Journal of immunological methods.

[84]  C. W. Tabor,et al.  Purification of amine oxidase from beef plasma. , 1954, The Journal of biological chemistry.

[85]  M. Dixon.  The determination of enzyme inhibitor constants. , 1953, The Biochemical journal.

[86]  D. Burk,et al.  The Determination of Enzyme Dissociation Constants , 1934 .

[87]  Sherine N. Khattab,et al.  Synthesis, Docking, and Evaluation of Antimicrobial Activity of a New Series of Acyclo C-Nucleosides of 1, 2, 4-Triazolo[4, 3-a]quinoxaline Derivatives , 2016 .

[88]  Thierry Kogej,et al.  Compound Properties and their Influence on Drug Quality , 2015 .

[89]  B. Winblad,et al.  The effect of age on the activity and molecular properties of human brain monoamine oxidase , 2005, Journal of Neural Transmission.

[90]  B. Mondovì,et al.  Amine oxidases and tumors. , 2004, Neurotoxicology.

[91]  F. Lombardo,et al.  Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. , 2001, Advanced drug delivery reviews.

[92]  J. Tolan,et al.  MDCK (Madin-Darby canine kidney) cells: A tool for membrane permeability screening. , 1999, Journal of pharmaceutical sciences.