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Synthesis and Anticancer Activity of New Hydrazide-hydrazones and Their Pd(II) Complexes



Hydrazones, one of the important classes of organic molecules, are pharmaceutical
agents comprising –CO-NH-N=CH- group in the structure therefore and exhibiting significant
biological activity.



5-Chloro-N’-[(substituted)methylidene] pyrazine-2-carbohydrazide (3a-g) and their Pd(II)
complexes (4a-h) were synthesized and investigated in vitro anticancer activity on A549, Caco2 cancer
and normal 3T3 fibroblast cell lines, using the MTT assay.



Anticancer activity screening results revealed that some compounds showed remarkable cytotoxic
effect. Among them, 5-chloro-N'-[(4-hydroxyphenyl)methylidene] pyrazine-2-carbohydrazide
(3c) displayed higher cytotoxic activity against A549 cancer cell line than the reference drug cisplatin.



Compound 3c showed high cytotoxic activity against A549 cancer cell line but it showed
low cytotoxic effect against normal 3T3 fibroblast cell line. Antiproliferative and antimetastatic effects
of 3c were determined by the real-time monitoring of cell proliferative system (RTCA DP). The cell
proliferation, metastatic and invasive activities of A549 cells were decreased due to increased concentration
of 3c.
