Synthesis and antiproliferative activity of the salicyl-based Weinreb amides and their derivatives in cancer cell lines

Abstract

A series of 11 pseudotripeptide Weinreb amides and 8 pseudodipeptide sulfonylhydrazides were synthesized and assessed using the resazurin-based method to determine their antiproliferative activity against the following cancer cell lines: lymphoblastic leukaemia (CEM), acute myeloid leukaemia (MV4-11), multiple myeloma (U266), and breast adenocarcinoma (MCF-7). The investigated compounds have shown a mid-micromolar range of inhibition. When L-Trp was included in the centre of the tripeptide chain, the derivatives exhibited a single-digit micromolar activity against the MV4-11 and U266 cell lines. Further immunoblotting experiments and caspase-3/7 activity assays for the most active compound 3e have confirmed apoptosis as the mechanism of cell death.