Cytotoxicity of Hydrazones of Morpholine Bearing Mannich Bases Towards Huh7 and T47D Cell Lines and Their Effects on Mitochondrial Respiration

Author(s): Kaan Kucukoglu, Halise Inci Gul, Mustafa Gul, Rengul Cetin-Atalay, Yosra Baratli, Bernard Geny

Journal Name: Letters in Drug Design & Discovery

Volume 13 , Issue 8 , 2016

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Graphical Abstract:


N,N’-bis[1-(substitutedphenyl)-3-(morpholine-4-yl)propylidene]hydrazine dihydrochlorides, N1-N11 were designed and synthesized as cytotoxic agents. These compounds were synthesized by the reaction of 2 moles of 1- (substitutedphenyl)-3-(morpholine-4-yl)-1-propanone hydrochlorides with 1 mole of hydrazine hydrate. The compounds reported here are new, except N1 and N4. The cytotoxicity of the compounds was tested against human hepatoma (Huh7) and breast cancer (T47D) cell lines. 5-Fluorouracil (5-FU) was used as a reference compound. It was found that N3, which has 4-methoxy substituent on phenyl ring, was the most cytotoxic compound towards both cell lines. Its cytotoxicity was 5.6 times higher than 5-FU. Representative compounds N2 at 144, 264 and 424 M and N3 at 401 M concentrations significantly inhibited mitochondrial respiration in a dose dependent manner in liver homogenates. This suggests that the inhibition of mitochondrial respiration may be one of the contributing mechanisms to the cytotoxicity of the compounds. N3 may serve as a candidate compound for further studies.

Keywords: Cytotoxic activity, Huh7, hydrazone, Mannich base, mitochondrial respiration, T47D.

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Article Details

Year: 2016
Page: [734 - 741]
Pages: 8
DOI: 10.2174/1570180813666160113002907
Price: $65

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