Cancer cell growth inhibition by aroylhydrazone derivatives

• Main Authors: Ivan Iliev, Darko Kontrec, Roumiana Detcheva, Maya Georgieva, Anelia Balacheva, Nives Galić, Tamara Pajpanova
• Format: Article
• Language: English
• Published: Taylor & Francis Group 2019-01-01
• Series: Biotechnology & Biotechnological Equipment
• Subjects: aroylhydrazones; nicotinic acid hydrazide; isonicotinic acid hydrazide; antiproliferative activity
• Online Access: http://dx.doi.org/10.1080/13102818.2019.1608302

Hydrazones have versatile properties that make them promising for a range of possible applications. In this study, we examined a library of 17 aroylhydrazones derived from nicotinic acid hydrazide (1-12) and isonicotinic acid hydrazide (A-E) created by us for their biological activity. The antiproliferative activity of the compounds was investigated on non-tumour MCF-10A cells and cancer cell lines, MCF-7 and MDA-MB-231. Four compounds were selected as most active in cell growth inhibition of the tumour cell lines. These compounds, 5, 11, C and E, were tested on four additional cell lines: non-tumour BJ and cancer cell lines, HeLa, HepG2 and HT-29. Compounds 5 and E exhibited the highest selectivity index on cancer cell lines MDA-MB-231, HeLa and HepG2. High selectivity to MCF-7 cells was demonstrated with compound 5. Compound C was very selective to HepG2 cells as well as to MDA-MB-231 but to a lesser degree. Compound 11 showed selectivity against MDA-MB-231. The obtained results allow assessing the structure–activity relationship of the compounds and provide insight into the further development of this group of aroylhydrazones as more potent and selective anti-neoplastic agents.