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

Molecules

卷:20

Ayman El-Faham¹  Sherine N. Khattab²  Hazem A. Ghabbour³  Hoong-Kun Fun³  Muhammad Farooq⁴  Mohammad A. Wadaan⁴  Nael Abutaha⁴ 

[1] Department of Chemistry, College of Science, King Saud University, P.O. Box 2455,Riyadh 11451, Saudi Arabia;

[2] Department of Chemistry, Faculty of Science, Alexandria University, P.O. Box 426,Alexandria 21321, Egypt;

[3] Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University,P.O. Box 2457, Riyadh 11451, Saudi Arabia;

[4] Department of Zoology, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia;

关键词: valproic acid;    isatin;    hydrazide-hydrazone;    anti-cancer activity;   

DOI  :  10.3390/molecules200814638

来源: DOAJ

【 摘 要 】

Eight novel N′-(2-oxoindolin-3-ylidene)-2-propylpentane hydrazide-hydrazone derivatives 4a–h were synthesized and fully characterized by IR, NMR (1H-NMR and13C-NMR), elemental analysis, and X-ray crystallography. The cyto-toxicity and in vitro anti-cancer evaluation of the prepared compounds have been assessed against two different human tumour cell lines including human liver (HepG2) and leukaemia (Jurkat), as well as in normal cell lines derived from human embryonic kidney (HEK293) using MTT assay. The compounds 3e, 3f, 4a, 4c, and 4e revealed promising anti-cancer activities in tested human tumour cells lines (IC50 values between 3 and 7 μM) as compared to the known anti-cancer drug 5-Fluorouracil (IC50 32–50 μM). Among the tested compounds, 4a showed specificity against leukaemia (Jurkat) cells, with an IC50 value of 3.14 μM, but this compound was inactive in liver cancer and normal cell lines.

【 授权许可】

Unknown