Cytotoxicity Assay on Several Theophylline-7-acetic Acid Amides with Amino Acids

نویسندگان

  • Y. Voynikov
  • G. Momekov
چکیده

Theophylline-7-acetic acid (7-TAA) derivatives with several amino acids were screened for antiproliferative effects on acute (HL-60) and chronic (K-562) myeloid leukemia cells as well as on non-malignant cells derived from embryonic human kidney (HEK 293T). The anti-proliferative effects (IC50) were revealed at relatively high concentrations, between 330.4 and 1051.9 μM, but the tested compounds proved to be devoid of cytotoxicity on HEK 293T in the evaluated concentration range (50-1200 μM). The amino acid esters demonstrated higher cytotoxicity towards the myeloid leukemia cells compared to the carboxylic acid derivatives.

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

A Computational Study of Cytotoxicity of Substituted Amides of Pyrazine-2-carboxylic acids Using QSAR and DFT Based Molecular Surface Electrostatic Potential

Pyrazine derivatives are important class of compounds with diverse biological and cytotoxic activities and clinical applications. In this study, B3 p 86 / 6 – 31 + + G * was used to compute and map the molecular surface electrostatic potentials of a group of substituted amides of pyrazine-2-carboxylic acids to identify common features related to their subsequent cytotoxicities. Several statisti...

متن کامل

A Computational Study of Cytotoxicity of Substituted Amides of Pyrazine-2-carboxylic acids Using QSAR and DFT Based Molecular Surface Electrostatic Potential

Pyrazine derivatives are important class of compounds with diverse biological and cytotoxic activities and clinical applications. In this study, B3 p 86 / 6 – 31 + + G * was used to compute and map the molecular surface electrostatic potentials of a group of substituted amides of pyrazine-2-carboxylic acids to identify common features related to their subsequent cytotoxicities. Several statisti...

متن کامل

Spectrophotometry of theophylline-7-acetic acid and theophylline.

A spectrophotometric assay procedure is described for individually measuring theophylline-7-acetic acid and theophylline in 2.0 ml of serum. Absorbance is a linear function of concentration over a range of 0.5-40 mg/liter for theophylline-7-acetic acid and 0.5-40 mg/liter for theophylline. No endogenous or exogenous compounds were found that interfere with theophylline-7-acetic acid determinati...

متن کامل

Potentiometric and Thermodynamic Studies of Binary and Ternary Transition Metal(II) Complexes of Imidazole-4-acetic Acid and Some Bio-relevant Ligands

Proton–ligand association constants of imidazole-4-acetic acid (IMA) were determined potentiometrically in aqueous solution at different temperatures in the range 15–35 C. The stepwise stability constants of IMA with some selected bivalent transition metal ions were also determined in 0.1 mol dm NaNO3. The stability of the complexes follows the trend Cu [ Ni [ Co [ Mn, which is in agreement wit...

متن کامل

Synthesis, gastroprotective effect and cytotoxicity of new amino acid diterpene monoamides and diamides.

Following our studies on the gastroprotective effect and cytotoxicity of terpene derivatives, new amides were prepared from the diterpene 8(17)-labden-15,19-dioic acid (junicedric acid) and its 8(9)-en isomer with C-protected amino acids (amino acid esters). The new compounds were evaluated for their gastroprotective effect in the ethanol/HCl-induced gastric lesions model in mice, as well as fo...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:

دوره   شماره 

صفحات  -

تاریخ انتشار 2014