Synthesis Of New Dehydropeptide Mimics Involving Some Heterocyclic Rings And Their Investigation As Cytotoxic Agents | 108877
Chemical Sciences Journal
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Dehydropeptides are significant constituents of several biologically
active peptides. Accordingly, the class compounds present are useful
synthetic precursors for assembling biologically active identities, namely,
cytotoxic agents. Relative to the main peptide chain, the existence of the SP2
hybridized ?-? atoms in the peptide chains limits the conformations of the
side chains to either Z or E orientation at the C? carbon atom. This decreases
the conformational flexibility, which makes the ?-? dehyrodropeptide
position and the amide backbone structurally suitable for building up some
heterocyclic rings. The heterocyclic rings are, consequently, embedded
in the peptide chain backbone as additional dehyro-peptidomimetics.
Considerable research works towards their synthesis; structural, as well
as, biological investigations are consequently, recently, explored. Herein,
we will focus upon the synthesis and characterization of some tetrazols
and oxadiazoles dehydro-peptidomimetics and their biological evaluation
as cytotoxic, namely, anticancer agents against MCF-7 human breast
carcinoma cells. The realized preliminary tests revealed that our nine
tested compounds demonstrated cytotoxicity which was somewhat dose
dependent. Five of them demonstrated high anticancer activity.
Atef AbdelMoniem Kalmouch has completed his PhD in the Faculty of Science at Zagazig University, Egypt. He is the Head of Peptide Chemistry Department, National Research Centre- Egypt. He has published more than 20 papers in reputed journals and has been serving as an Editorial Board Member of repute journals.