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

Molecules

Ayman El-Faham¹  Muhammad Farooq³  Sherine N. Khattab²  Nael Abutaha³  Mohammad A. Wadaan³  Hazem A. Ghabbour⁴  Hoong-Kun Fun⁴ 

[1] Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia;Department of Chemistry, Faculty of Science, Alexandria University, P.O. Box 426, Alexandria 21321, Egypt; E-Mail:;Department of Zoology, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia; E-Mails:;Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia; E-Mails:

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

DOI  :  10.3390/molecules200814638

来源: mdpi

【 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 and ¹³C-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】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.