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Cytotoxic Evaluation (cytotoxic + evaluation)
Selected AbstractsSynthesis 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 Evaluation of 6-(3-Pyrazolylpropyl) Derivatives of 1,4-Naphthohydroquinone-1,4-diacetateARCHIV DER PHARMAZIE, Issue 10 2009Aurora Molinari Abstract Several new 6-(3-pyrazolylpropyl) derivatives of 1,4-naphthohydroquinone-1,4-diacetate (NHQ-DA) have been prepared by chemical modifications of the Diels,Alder adduct of ,-myrcene and 1,4-benzoquinone. All these new compounds and precursors have been evaluated in vitro for their cytotoxicity against cultured human cancer cells of MB-231 breast-adeno carcinoma, A-549 lung carcinoma, and HT-29 colon carcinoma. GI50 values ranged in and below the micromolar concentration level. [source] ChemInform Abstract: Synthesis and in vitro Cytotoxic Evaluation of New Derivatives of Pyrido[1,2-a]benzimidazolic Ring System: The Pyrido[1,,2,:1,2]imidazo[4,5-h]quinazolines.CHEMINFORM, Issue 7 2002Marianne Dupuy Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Enantioselective Synthesis and Cytotoxic Evaluation of 4,5-Dihydro-5-[aryl(hydroxy)methyl]-3-methylidenefuran-2(3H)-onesCHEMISTRY & BIODIVERSITY, Issue 9 2005Tomasz Janecki A series of enantiomerically enriched 4,5-dihydro-5-[aryl(hydroxy)methyl]-3-methylidenefuran-2(3H)-ones (8) were synthesized by means of asymmetric Sharpless dihydroxylation of the 2-phosphorylated 5-aryl-pent-4-enoic acids 13, followed by Horner,Wadsworth,Emmons reaction of the resulting furanones 15 (Scheme,2). An enantiomeric excess (ee) of 20,95% was achieved for compounds 8, and their absolute configurations were determined by the Mosher ester method. Cytotoxic evaluation against L-1210 and HL-60 leukemia cell lines revealed that the target compounds 8 are active in the micromolar concentration range (Table,2). Thereby, significant differences in activity between the corresponding enantiomers were observed for the HL-60 cell line. [source] Cytotoxic evaluation of injectable cyclodextrin nanoparticlesJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 5 2006Erem Memisoglu-Bilensoy Nanoparticles were prepared using ,-CDC6, which is an amphiphilic , -cyclodextrin derivative modified on the secondary face with 6C aliphatic esters. A nanoprecipitation technique was used to prepare the blank nanoparticles without any surfactant and nanoparticles containing Pluronic F68 as surfactant in a concentration range of 0.1 to 1%. Nanoparticle formulations were characterized by particle size distribution and zeta potential measurements. Entrapment efficiency and in-vitro release profiles were determined and the cytotoxicity of these injectable nanospheres was evaluated against mouse fibroblast L929 cell line and human polymorphonuclear cells by methlythiazolyltetrazolium assay. As far as particle size and zeta potential are concerned, there is a relationship between surfactant presence and nanoparticle characteristics. However, these effects are not significant. It was also found that surfactant presence has no effect on model drug nimodipine encapsulation but accelerates the in-vitro release of the drug. Cell culture studies on mouse fibroblasts and human polymorphonuclear cells revealed a concentration-dependent cytotoxicity more pronounced in fibroblast cells. This led to the conclusion that the use of surfactants in injectable nanoparticles prepared from amphiphilic ,-cyclodextrins may lead to altered in-vitro properties and impaired safety for the drug delivery system. [source] Enantioselective Synthesis and Cytotoxic Evaluation of 4,5-Dihydro-5-[aryl(hydroxy)methyl]-3-methylidenefuran-2(3H)-onesCHEMISTRY & BIODIVERSITY, Issue 9 2005Tomasz Janecki A series of enantiomerically enriched 4,5-dihydro-5-[aryl(hydroxy)methyl]-3-methylidenefuran-2(3H)-ones (8) were synthesized by means of asymmetric Sharpless dihydroxylation of the 2-phosphorylated 5-aryl-pent-4-enoic acids 13, followed by Horner,Wadsworth,Emmons reaction of the resulting furanones 15 (Scheme,2). An enantiomeric excess (ee) of 20,95% was achieved for compounds 8, and their absolute configurations were determined by the Mosher ester method. Cytotoxic evaluation against L-1210 and HL-60 leukemia cell lines revealed that the target compounds 8 are active in the micromolar concentration range (Table,2). Thereby, significant differences in activity between the corresponding enantiomers were observed for the HL-60 cell line. [source] | ||||||||||