Antiproliferative Properties of Vinyl Dipeptides: Synthesis and MCF-7 Cell Line Testing
Open Access
- 1 January 2012
- journal article
- Published by Scientific Research Publishing, Inc. in Open Journal of Medicinal Chemistry
- Vol. 02 (04), 105-111
- https://doi.org/10.4236/ojmc.2012.24013
Abstract
Peptide mimics derived with close structure to peptide have vast utility because they are expected to interfere with biological targets while having superior drug-like properties if compared to peptides. In this work, novel vinyl dipeptides which are different in a double bond between the α-carbon of peptide and C1 of its side chain. Added to that, suitable substituents were selected to harness drug-like properties. The compounds were found to have moderate activities when tested against MCF-7 breast cancer cell line. For instance, the adamantyl analogue 2-(benzoylamino)-3-(2-furyl)-N-(1-adamantyl) propenamide (1c) and the heterocyclic analogue 2-(Benzoylamino)-3-(2-furyl)-N-[2-(5-cyanothia-zol-2-yl)] propenamide (1o) exhibited inhibition potency at 27.4 and 37.8 μM, respectively.Keywords
This publication has 14 references indexed in Scilit:
- Pharmacological Promiscuity and Molecular PropertiesPublished by Wiley ,2012
- Identification of plasmepsin inhibitors as selective anti-malarial agents using ligand based drug designBioorganic & Medicinal Chemistry Letters, 2011
- Virtual screening identification of novel severe acute respiratory syndrome 3C-like protease inhibitors and in vitro confirmationBioorganic & Medicinal Chemistry Letters, 2011
- Aminocarbonyl Arylvinylbenzamides as Gastric Sparing Anti‐inflammatory AgentsArchiv der Pharmazie, 2011
- Anticonvulsant and acute neurotoxic effects of imperatorin, osthole and valproate in the maximal electroshock seizure and chimney tests in mice: A comparative studyEpilepsy Research, 2009
- Discovery of Geranylgeranyltransferase-I Inhibitors with Novel Scaffolds by the Means of Quantitative Structure−Activity Relationship Modeling, Virtual Screening, and Experimental ValidationJournal of Medicinal Chemistry, 2009
- Optimizing Dvl PDZ domain inhibitor by exploring chemical spaceJournal of Computer-Aided Molecular Design, 2008
- Design and Synthesis of Novel Bioactive Peptides and PeptidomimeticsJournal of Medicinal Chemistry, 2003
- Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settingsAdvanced Drug Delivery Reviews, 2001
- New Colorimetric Cytotoxicity Assay for Anticancer-Drug ScreeningJNCI Journal of the National Cancer Institute, 1990