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

The anti-cancer profile of newly synthesized compounds was also tested against leukaemia cells (Jurkat cells, originated from human T lymphocytes). The compound 4c was most active, with an IC50 value of just 2.90 ± 36.3 μM, which was much lower than the positive control (5-FU IC50 = 51.16 ± 47.4 μM). Similarly, the compounds 3f, 4a, and 4c showed strong activity and IC50 values were much lower as compared to 5-FU (Table 3 and Figure 5 ). The order of activity was 3f, 4a, 4e, and 3e in ascending order (Table 3 and Figure 5 ). The compound 1 showed a weaker level of activity against Jurkat cells (IC50 79.35 ± 40.7 μM) and, indeed, this was much weaker than 5-FU (IC50 51.16 ± 47.4 μM). Finally the cyto-toxicities of these compounds were screened in the normal human embryonic kidney (HEK293) cell line, in order to assess whether these compounds are active only in cancer cells or whether they possess toxicity against normal cells as well. The results revealed that the compound 4c turned out to be most toxic by disrupting the cell survival of normal cells (HEK 293) with IC50 4.77 ± 42.7 μM. The compounds 3a, 4b, and 4g also possessed some level of cyto-toxicity against HEK 293 cells with IC50 values 16.73 ± 50.0, 26.08 ± 31.3, and 45.43 ± 48.9 μM, respectively. The IC50 values of these compounds in HEK cells, however, are much higher compared to their activity in cancer cells (Table 3 and Figure 5 ). The compounds 3e, 3f, 4a, and 4e showed no activity in HEK 293 cells, but strong activity in liver (HepG2) and leukaemia (Jurkat) cancer cells, suggesting that these compounds are potent and potentially viable anti-cancer molecules.