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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 as
antiproliferative agents.
Aims: We have identified a series of arylpiperazine derivatives acting as PAR1 antagonists; the selected molecules have been evaluated for their antiproliferative properties.
Method: All the compounds inhibited the growth of a panel of cell lines expressing
PAR1; two of them, compounds 13 and 15, were able to inhibit, in a dose dependent manner, the growth of the selected cell lines with the lowest IC50 values, and were further characterized to define the mechanism responsible for the observed antiproliferative effect.
Result: This study
directed us to the identification of two interesting leads that may help to further validate PAR1 as an important therapeutic target for cancer treatment.
| Authors: | Ilaria Zotti, Andrea; Di Gennaro, Elena; Corvino, Angela; Frecentese, Francesco; Magli, Elisa; Perissutti, Elisa; Cirino, Giuseppe; Roviezzo, Fiorentina; Terranova-Barberio, Manuela; Iannelli, Federica; Caliendo, Giuseppe; Santagada, Vincenzo; Fiorino, Ferdinando; Budillon, Alfredo; Severino, Beatrice | |
| Journal: | Anti-Cancer Agents in Medicinal Chemistry | |
| DOI: | 10.2174/1871520616666160926120904 |
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 was ... more
Synthesis and Evaluation of Cytotoxic Activity of Some Pyrroles and Fused Pyrroles
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 pyrro ... more
Design and Synthesis of 1,4-dihydropyridine Derivatives as Anti-cancer Agent
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 ... more
Synthesis of medicinally privileged heterocycles through dielectric heating
Heterocyclic compounds are enormously crucial in various industries including food, agricultural, cosmetics and pharmaceuticals. Heterocyclic pharmacophores are one of the main chemical components in drug discovery research. A report in 2013 claims that four out of six and nine out of twent ... more
Targeting the PI3K/AKT/mTOR pathway in prostate cancer development and progression
Dr Claudio Festuccia (University of L'Aquila, Italy) discusses experimental and clinical data on the pharmacological inhibition of the Akt/mTOR pathways. These pathways play a key role in the modulation of cellular proliferation, tumor growth and survival through phosphorylation of differen ... more
Investigating plasma levels as a biomarker for Alzheimer's disease
A Centre for Healthy Brain Ageing (CHeBA) paper presents the first detailed study of the relationship between plasma levels of two amyloid beta peptides (Aβ1-40 and Aβ1-42), brain volumetrics (measures studying the size of brain, which shrinks with Alzheimer's disease) and cognitive perform ... more
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