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.