Four suberoylanilide hydroxamic acid (SAHA) derivatives (N34, N4I, N4B, N24) were designed and
synthesized on the basis of our previous studies on N25. Assays for anti-proliferative activity and histone
deacetylase (HDAC) activity were performed against human lung cancer (SPC-A-1, LTEP-a-2, NCI-H1650) and
normal lung cells (MRC-5), which were compared with those of SAHA. Molecular docking was used to
theoretically confirm the receptor-binding ability of N34. Ultimately, N34 was validated as the best HDAC
inhibitor candidate. Furthermore, the effects of N34 on the levels of apoptosis- and autophagy-associated proteins
caspase-3, caspase-9, Bcl-2 and Beclin-1 in SPC-A-1 cells were evaluated. N34 exerted more evident effects on
human lung cancer than the other three SAHA derivatives did.
Keywords: Anti-proliferative activity, apoptosis- and autophagy-associated protein, HDAC activity assay, suberoylanilide hydroxamic acid
(SAHA) derivaties, synthesis.
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