Synthesis and Cytotoxicity of Novel 3-Aryl-1-(3'-dibenzylaminomethyl-4'-hydroxyphenyl)-propenones and Related Compounds

スポンサーリンク

概要

• 論文の詳細を見る

• The reaction of various 4'-hydroxychalcones (1a-e) with paraformaldehyde and dibenzylamine led to the formation of a novel series of 4'-hydroxy-3'-dibenzylaminomethyl chalcones (7a-e) instead of 4'-hydroxy-3',5'-bis-(dibenzylaminomethyl)chalcones 4. In order to rationalise the formation of monoadduct 7, energy minimized model structures of 4a and 7a were compared. The in vitro cytotoxic activities of 7a-e were tested against PC-3 cell lines for the first time in this study and compared with the precursor 4'-hydroxychalcones (1a-e). Except for compound 7a (IC_<50>: 19.85μM), insertion of dibenzylaminomethyl function into 4'-hydroxychalcones resulted in complete loss of cytotoxic activity. The results suggested that it is not only the pK_a but also the shape and size of the amine that is critical in governing the cytotoxic activity.

• 公益社団法人日本薬学会の論文
• 2008-12-01

著者

• Li Pui-kai

  Division Of Medicinal Chemistry And Pharmacognosy College Of Pharmacy The Ohio State University

• Li Pui-kai

  Division Of Medicinal Chemistry And Pharmacognosy College Of Phamacy The Ohio State University

• GuL Halise

  Department of Pharmaceutical Chemistry, Faculty of Pharmacy Ataturk University

• Gul Halise

  Department Of Pharmaceutical Chemistry Faculty Of Pharmacy Ataturk University

• GuL Mustafa

  Department of Physiology, Faculty of Medicine, Ataturk University

• Gul Mustafa

  Department Of Clinical Microbiology Kahramanmaras Sutcu Imam University Faculty Of Medicine

• PANDIT Bulbul

  Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University

• YERDELEN Kadir

  Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ataturk University

• DAS Umashankar

  College of Pharmacy and Nutrition, University of Saskatchewan

• DIMMOCK Jonathan

  College of Pharmacy and Nutrition, University of Saskatchewan

• Pandit Bulbul

  Division Of Medicinal Chemistry And Pharmacognosy College Of Pharmacy The Ohio State University

• Das Umashankar

  College Of Pharmacy And Nutrition University Of Saskatchewan

• Yerdelen Kadir

  Department Of Pharmaceutical Chemistry Faculty Of Pharmacy Ataturk University

• Dimmock Jonathan

  College Of Pharmacy And Nutrition University Of Saskatchewan

関連論文

• Antifungal Evaluation of Bis Mannich Bases Derived from Acetophenones and Their Corresponding Piperidinols and Stability Studies(Pharmacology)
• Beneficial Effects of Hippophae rhamnoides L. on Nicotine Induced Oxidative Stress in Rat Blood Compared with Vitamin E
• Anti-inflammatory Activity of Bis(3-aryl-3-oxo-propyl)methylamine Hydrochloride in Rat(Pharmacology)
• Cytotoxicity of Some Azines of Acetophenone Derived Mono-Mannich Bases against Jurkat Cells
• New curcumin analogues exhibit enhanced growth-suppressive activity and inhibit AKT and signal transducer and activator of transcription 3 phosphorylation in breast and prostate cancer cells
• Synthesis and Cytotoxicity of Novel 3-Aryl-1-(3'-dibenzylaminomethyl-4'-hydroxyphenyl)-propenones and Related Compounds
• Synthesis and Pharmacological Analysis of High Affinity Melatonin Receptor Ligands
• Intraperitoneal Tenoxicam to Prevent Abdominal Adhesion Formation in a Rat Peritonitis Model
• α-Substituted 1-Aryl-3-dimethylaminopropanone Hydrochlorides : Potent Cytotoxins towards Human WiDr Colon Cancer Cells
• Urinary Tract Infection Aggravates Oxidative Stress in Diabetic Patients
• Hippophae rhamnoides L. : chromatographic methods to determine chemical composition, use in traditional medicine and pharmacological effects
• Effects of Putative Hydroxylated Thalidomide Metabolites on Blood Vessel Density in the Chorioallantoic Membrane (CAM) Assay and on Tumor and Endothelial Cell Proliferation

もっと見る 閉じる

スポンサーリンク