Preliminary in vitro evaluation of the anti-proliferative activity of guanylhydrazone derivatives

Abstract

Preliminary in vitro evaluation of the anti-proliferative activity of guanylhydrazone derivativesGuanylhydrazones have shown promising antitumor activity in preclinical tumor models in several studies.In this study, we aimed at evaluating the cytotoxic eff ect of a series of synthetic guanylhydrazones. Diff erent human tumor cell lines, by including HCT-8 (colon carcinoma), MDA-MB-435 (melanoma) and SF-295 (glioblastoma) were continuous exposed to guanylhydrazone derivatives for 72 hours and growth inhibition of tumor cell lines and macrophages J774 was measured using tetrazolium salt (MTT) assay. Compounds 7, 11, 16 and 17 showed strong cytotoxic activity with IC 50 values lower than 10 μmol L -1 against four tumor cell lines. Among them, 7 was less toxic to non-tumor cells. Finally, obtained data suggest that guanylhydrazones may be regarded as potential lead compounds for the design of novel anticancer agents.

Electrochemical Evaluation of Aminoguanidine Hydrazone Derivative with Potential Anticancer Activity: Studies of Glassy Carbon/CNT and Gold Electrodes Both Modified with PAMAM

“…The analytical grade reagents were purchased from Sigma-Aldrich, Acros Chemical Co. or Merck. The substance LQM10 (2E)-2-(3,5-di-tert-butyl-4-hydroxybenzylidene)hydrazinecarboximidamide was synthesized using a previously described procedure [8].…”

“…Aminoguanidine hydrazine derivatives are bioactive compounds that have been intensively studied for their different (and interesting) biological activities, such as in the treatment of hypertension (Guanabenz) [1] [2] [3], or antiarrhythmic [4] [5]; nonpeptide NPFF1 Receptor Antagonists reverse opioid-induced hyperalgesia [6]; as modulators of norfloxacin resistance in S. aureus that overexpress the efflux pump of NorA [7]; and anticancer [8].…”

“…They are derived from the same chemical group as aminoguanidine, so it has mixed properties (receptor and donor) in the formation of hydrogen bonds. Its anticancer agent properties were recently highlighted, but the molecules of this class have solubility in aqueous solutions that can be considered low [8]. Studies the association of this class the compound with some carriers as cyclodextrin, liposomes or linear polymers were few reported [9].…”

Aminoguanidine hydrazones (AGH's) as modulators of norfloxacin resistance in Staphylococcus aureus that overexpress NorA efflux pump

“…The title compounds were isolated after cooling to room temperature, being washed, or recrystallized using an appropriate solvent. Structural characterization of the products is described elsewhere [20,21]. LogP was calculated in the Hy-perChem™ software Release 8.0.8 Windows.…”

Development and Validation of HPLC-DAD and UHPLC-DAD Methods for the Simultaneous Determination of Guanylhydrazone Derivatives Employing a Factorial Design

“…They concluded that the 3-nitrophenyl and 4-nitrophenyl moieties are important pharmacophore groups which increase the affinity for specific tumor receptors [ 11 ]. Other research groups have synthesized new guanylhydrazones with anticancer activity in order to obtain new molecules for the treatment of this disease [ 12 ]. The guanylhydrazone derivatives 2-[(3,5-di- tert -butyl-4-hydroxyphenyl)methylene]hydrazinecarboximidamide (LQM10), 2-([1,10-biphenyl]4-ylmethylene)hydrazinecarboximidamide (LQM14) and 2-[(3,4-dichlorophenyl)-methylene]hydrazinecarboximidamide (LQM17) have shown pharmacological activity against some neoplastic cell lines, such as human colon (HCT-8), melanoma (MDA-MB435), glioblastoma (SF-295) and promyelocytic leukemia (HL-60) [ 12 ].…”