Synthesis and antiproliferative activity of novel neocryptolepine-hydrazides hybrids

By combining the structural features of neocryptolepine and hydrazides, novel hybrid compounds 8a-d and 9a-j were synthesized using a simple and convenient method. Evaluation of these compounds against human hepatocellular carcinoma (HepG₂) cell line using MTT assay was performed. Compound 8c was identified as the most active anticancer agent as it showed effectiveness at low concentration with IC₅₀ 2.51 μM on the tested cell line when compared with reference drug 5-FU. It is worth to note that all tested compounds showed antiproliferative activity at very lower micro molar concentrated when compared with the reference drug except compounds 9a, 9e, and 9j which were less active than 5-FU. The anticancer screening results of the tested compounds provide an encouraging framework that could lead to the development of potent new anticancer agents based on neocryptolepine core structure.