Synthesis, Characterization, and Anti-Cancer Activity of Some New N'-(2-Oxoindolin-3-ylidene)-2-propylpentane hydrazide-hydrazones Derivatives

El-Faham, Ayman; Farooq, Muhammad; Khattab, Sherine N.; Abutaha, Nael; Wadaan, Mohammad A.; Ghabbour, Hazem A.; Fun, Hoong-Kun

In conclusion, the screening results from human cancer and normal cell lines suggested that isatin derivatives were remarkably influenced by various substituents on the isatin ring and at the N-terminal of the hydrazide-hydrazone moiety. The data revealed that replacement of N-hydrogen at position 1 of the isatin moiety 3a by methyl and benzyl of the targeted compound (3e and 3f) noticeably enhanced the activity against the selected two cell lines, HepG2 and Jurkat, for compound 3f. The presence of the valproic acid moiety as hydrazide-hydrazone derivatives 4a make the compound more targeted towards Jurakt cells in vitro. Introducing the chlorine atom to the molecule 4c, meanwhile, increased the reactivity more significantly than with 4a and 3a towards the three cell lines HepG2, Jurkat, and HEK293. Furthermore, the methyl group in the same analogous compound 4e increased the reactivity towards the two cell lines HepG2 and Jurkat more than the benzyl group 4f. The rest of the compounds had no effect on the three cell lines. Further studies to assess the effect of more derivatives on various cancer cell biomarkers are currently underway in our lab.