Home About us Contact
|
Home About us Contact | ||
|
|
||
In-vitro Cytotoxic Activity (in-vitro + cytotoxic_activity)
Selected AbstractsSynthesis, DNA-Binding, Cleavage, and Cytotoxic Activity of New 1,7-Dioxa-4,10-diazacyclododecane Artificial Receptors Containing Bisguanidinoethyl or Diaminoethyl Double Side ArmsCHEMISTRY - A EUROPEAN JOURNAL, Issue 34 2007Xin Sheng Abstract Novel 1,7-dioxa-4,10-diazacyclododecane artificial receptors with two pendant aminoethyl (3) or guanidinoethyl (4) side arms have been synthesized. Spectroscopy, including fluorescence and CD spectroscopy, of the interactions of 3, 4, and their copper(II) complexes with calf thymus DNA indicated that the DNA binding affinity of these compounds follows the order Cu2+,4>Cu2+,3>4>3, and the binding constants of Cu2+,3 are Cu2+,4 are 7.2×104 and 8.7×104,M,1, respectively. Assessment by agarose gel electrophoresis of the plasmid pUC,19 DNA cleavage activity in the presence of the receptors showed that the complexes Cu2+,3 and Cu2+,4 exhibit powerful supercoiled DNA cleavage efficiency. Kinetic data of DNA cleavage promoted by Cu2+,3 and Cu2+,4 under physiological conditions fit to a saturation kinetic profile with kmax values of 0.865 and 0.596,h,1, respectively, which give about 108 -fold rate acceleration over uncatalyzed supercoiled DNA. This acceleration is due to efficient cooperative catalysis of the copper(II) center and the functional (diamino or bisguanidinium) groups. In-vitro cytotoxic activities toward murine melanoma B16 cells and human leukemia HL-60 cells were also examined: Cu2+,4 shows the highest activity with IC50 values of 1.62×10,4 and 1.19×10,5,M, respectively. [source] Novel Thiophenes, Thienopyrimidines, and Triazolothienopyrimidines for the Evaluation of Anticancer and Augmentation Effects of ,-RadiationARCHIV DER PHARMAZIE, Issue 7 2010Mohamed A. Shaaban Abstract New derivatives of thiophenes 2, 12, iminoaminothieno[2,3- d]pyrimidines 3, 5, and 6, triazolothieno[2,3- d]pyrimidines 8,11, pyrazolo- and triazinothieno[2,3- d]pyrimidines 4, 7, respectively, have been prepared by different synthetic procedures. Structure elucidation of the newly synthesized compounds was carried out via elemental analyses and spectral data. The antitumor activity of compounds 2, 3, and 9,12 was evaluated against in-vitro cell lines (HEPG-2 and MCF-7). Compounds 2, 3, 10, 11, and 12 showed significant in-vitro cytotoxic activity against hepatocellular carcinoma (HEPG-2) compared to the reference drug Doxorubicin. Compound 2 showed significant in-vitro cytotoxic activity against breast cancer (MCF-7) cells compared to the reference drug Doxorubicin. The augmenting effect of ,-radiation was assessed; here, compounds 2, 3, 10, and 11 showed the most potent in-vitro anticancer activity. [source] Synthesis and in-vitro Cytotoxic Evaluation of Novel Pyridazin-4-one DerivativesARCHIV DER PHARMAZIE, Issue 5 2010Souad Mojahidi Abstract A new series of N -aryl-4-oxo-1,4-dihydro-pyridazine-3-carboxylic acids has been synthesized by condensation of aryldiazonium with 4-hydroxy-6-methyl-2-pyrone. Some of these compounds exhibited in-vitro cytotoxic activity with moderate to excellent growth inhibition against the murine P815 mastocytoma cell line. Compound 5b showed an important cytotoxic activity against cell line P815 (IC50 = 0.40 ,g/mL). [source] Synthesis and Cytotoxic Activity of Novel Amidine Analogues of Bis(2-chloroethyl)amineARCHIV DER PHARMAZIE, Issue 8 2009Krzysztof Bielawski Abstract Novel nitrogen mustard agents 7,12 involving 4-(N,N -bis(2-chloroethyl)aminophenyl)propylamine linked to a 5-(4- N -alkylamidinophenyl)-2-furancarboxylic acid moiety by the formation of an amide bond have been synthesized, characterized, and evaluated for their in-vitro cytotoxic activity against MDA-MB-231 and MCF-7 human breast cancer cells. Evaluation of the cytotoxicity of 7,12 employing a MTT assay and inhibition of [3H]thymidine incorporation into DNA demonstrated that these compounds exhibit remarkable cytotoxic effects in comparison with 4-[bis(2-chloroethyl)amino]benzenebutanoic acid. Compounds 7 and 9, which possess a cationic amidine and 4,5-dihydro-1H -imidazol function moiety are approximately ten times more potent than 4-[bis(2-chloroethyl)amino]benzenebutanoic acid. The new compounds were evaluated as DNA topoisomerase II inhibitors. The cytotoxicity of the compounds 7,12 correlates with their DNA-binding affinities and their relative potency as topoisomerase II inhibitors. [source] | ||||||||||