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Mechanism and Anticancer Activity of the Metabolites of an Endophytic Fungi from Eucommia ulmoides Oliv

28.06.2017 | Li, Qi; Zhang, Yan; Shi, Jun-Ling; Wang, Yi-Lin; Zhao, Hao-Bin; Shao, Dong-yan; Huang, Qing-Sheng; Yang, Hui; Jin, M ..., Anti-Cancer Agents in Medicinal Chemistry , 2017

Abstract: Backgroud: Pinoresinol (Pin) and pinoresinol monoglucoside (PMG) are plant-derived lignan molecules with multiple functions. We showed previously that an endophytic fungus from Eucommia ulmoides Oliv., Phomopsis sp. XP-8 is able to produce Pin and PMG. Objective: This study ...


Synthesis and Evaluation of Cytotoxic Activity of Some Pyrroles and Fused Pyrroles

28.06.2017 | S. Fatahala, Samar; S. Mohamed, Mosaad; Youns, Mahmoud; H. Abd-El Hameed, Rania, Anti-Cancer Agents in Medicinal Chemistry , 2017

Abstract: Aims: Pyrrole derivatives represent a very interesting class as biologically active compounds. The objective of our study was to investigate the cytotoxic and apoptotic effects and antioxidant activity of the newly synthesized pyrrole derivatives. Method: A series of novel ...


Synthesis of Arylpiperazine Derivatives as Protease Activated Receptor 1 Antagonists and Their Evaluation as Antiproliferative Agents

28.06.2017 | Ilaria Zotti, Andrea; Di Gennaro, Elena; Corvino, Angela; Frecentese, Francesco; Magli, Elisa; Perissutti, Elisa; Ci ..., Anti-Cancer Agents in Medicinal Chemistry , 2017

Abstract: Background: Protease activated receptor-1 (PAR1) is a G-coupled receptor activated by α-thrombin and other proteases. Several reports have demonstrated the PAR1 involvement in tumorigenesis and tumor progression. In order to investigate on potential use of PAR1 antagonists ...


Design and Synthesis of 1,4-dihydropyridine Derivatives as Anti-cancer Agent

28.06.2017 | Viradiya, Denish; Mirza, Sheefa; Shaikh, Faraz; Kakadiya, Rajesh; Rathod, Anand; Jain, Nayan; Rawal, Rakesh; Shah, A ..., Anti-Cancer Agents in Medicinal Chemistry , 2017

Abstract: Aims: A series of 1,4-dihydropyridine based compounds bearing benzylpyridinium moiety have been designed and evaluated for in vitro anticancer activity against glioblastoma U87MG, lung cancer A549 and colorectal adenocarcinoma Caco-2 cell lines using the MTT assay. Method: Among these ...


Discovery of New Aminosubstituted Pyrrolopyrimidines with Antiproliferative Activity Against Breast Cancer Cells and Investigation of their Effect Towards the PI3Kα Enzyme

28.06.2017 | Daniilides, Konstantinos; Lougiakis, Nikolaos; Evangelidis, Thomas; K. Kostakis, Ioannis; Pouli, Nicole; Marakos, Pa ..., Anti-Cancer Agents in Medicinal Chemistry , 2017

Abstract: Objective: A series of novel 2,4-diaminosubstituted pyrrolo[3,2-d]pyrimidines was synthesized together with their corresponding 7-phenyl or 7-isopropyl counterparts. Results: Among the target derivatives, the 7-substituted analogues exhibited interesting cytotoxic activity against a ...


Evaluation of Melatonin Effect on Human Breast Cancer Stem Cells Using a Threedimensional Growth Method of Mammospheres

28.06.2017 | Ramos Lopes, Juliana; da Silva Kavagutti, Mayume; Arthur Faustino de Medeiros, Felipe; Aparecida Pires de Campos Zuc ..., Anti-Cancer Agents in Medicinal Chemistry , 2017

Abstract: Background: The high rates of women's death from breast cancer occur due to acquired resistance by patients to certain treatments, enabling the recurrence and/or tumor growth, invasion and metastasis. It has been demonstrated that the presence of cancer stem cells in human tumors, ...


TGF-β Signal Transduction in Pancreatic Carcinoma Cells is Sensitive to Inhibition by the Src Tyrosine Kinase Inhibitor AZM475271

28.06.2017 | Bartscht, Tobias; Rosien, Benjamin; Rades, Dirk; Kaufmann, Roland; Biersack, Harald; Lehnert, Hendrik; Ungefroren, H ..., Anti-Cancer Agents in Medicinal Chemistry , 2017

Abstract: Background: Earlier results from our group have shown that in pancreatic ductal adenocarcinoma (PDAC)-derived cells transforming growth factor (TGF)-β1-dependent epithelial-mesenchymal transition (EMT) and cell motility was inhibited by the Src inhibitors PP2 and PP1 both of ...


Biodegradable Polymer Hydrogels Based in Sorbitol and Citric Acid for Controlled Release of Bioactive Substances from Plants (Polyphenols)

13.06.2017 | S. Palencia, Manuel; A. Mora, Mayra; L Palencia, Sixta, Chemical Biology, 2017

Abstract: Background: Polyphenols are secondary metabolites of plants which are generally associated with the protection against ultraviolet radiation and aggression by pathogens. Epidemiological studies suggest that long term consumption of diets rich in plant polyphenols offer protection ...


Dehydroleucodine Induces a TP73-dependent Transcriptional Regulation of Multiple Cell Death Target Genes in Human Glioblastoma Cells

13.06.2017 | A. Ratovitski, Edward, Anti-Cancer Agents in Medicinal Chemistry , 2017

Abstract: Background: Dehydroleucodine, a natural sesquiterpene lactone from Artemisia douglassiana Besser (Argentine) and Gynoxys verrucosa (Ecuador). Objective: To define the molecular mechanisms underlying the effect of dehydroleucodine on the human glioblastoma cells. Method: ...


Crystallization and Preliminary X-ray Diffraction Analysis of CsaA from P. torridus: A Chaperone Rarely Found in Archaea

13.06.2017 | Sharma, Archana; K. Pal, Ravi; Goel, Manisha, Chemical Biology, 2017

Abstract: Background and Objective: CsaA is a molecular chaperone known to prevent aggregation of preproteins and also involved in the post-translational translocation of the proteins across the cytoplasmic membrane after correct folding. CsaA is known to be present in prokaryotes but is ...


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