TITLE:
Antiproliferative Properties of Vinyl Dipeptides: Synthesis and MCF-7 Cell Line Testing
AUTHORS:
Ashraf Hassan Bayoumi
KEYWORDS:
Piptidomimetics; Vinyl Dipeptides; 2-Aminopropenamide; Antiproliferative; Breast Cancer; Furan Derivatives
JOURNAL NAME:
Open Journal of Medicinal Chemistry,
Vol.2 No.4,
December
13,
2012
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.