54 research outputs found
N,M’(4,5-dihydro-1h-imidazol-2-yl)3-aza-1,10-decane-diamine and N,N’(4,5-dihydro-1h-imidazol-2-yl)3-aza-1,10-dodecane-diamine antagonize cell proliferation as selective ligands towards topoisomerase II
New alkyl imidazoline derivatives have been synthesized as potential anti-cancer agents. The anti-proliferative activity of these compounds, evaluated against representative human haematological and solid neoplastic cell lines, showed that N, N'-di (4,5-dihydro-1H-imidazol-2-yl)3-aza-1,10-decane-diamine (8) and N, N'-di (4,5-dihydro-1H-imidazol-2-yl)3-aza-1,10-dodecane-diamine (9) were the most active compounds; in fact, they inhibited the cell proliferation at submicromolar concentrations. In enzyme assays, compound 9 turned out to be an inhibitor of topoisomerase II at concentrations comparable with those of the reference topoisomerase II inhibitor, etoposide
Synthesis and antiproliferative activity of 3-aryl-2-[1H(2H)-benzotriazol-1(2)-yl]acrylonitriles variously substituted:Part 4
A new series of variously substituted 3-aryl-2-[1H(2H)-benzotriazol-1(2)-yl]acrylonitriles was synthesized and tested for antiproliferative and antitubercular activity as part of our continuing research program in the antimicrobial and antitumor fields. The most cytotoxic derivatives (5a,g,i,j,l and 7b) (CC50 < 3.0 microM against MT-4 cells) were evaluated against a panel of human cell lines derived from hematological and solid tumors, using 6-mercaptopurine (6-MP) and etoposide as reference drugs. In particular, E-2-(5,6-dimethyl-1H-benzotriazol-1-yl)-3-(3-nitrophenyl)acrylonitrile (5g) resulted more potent than 6-MP on all cell lines, even if 2-14-fold less potent than etoposide. In the antitubercular screening, the derivatives 5i,j and 7e showed moderate activity against some resistant strains of Mycobacterium tested
Synthesis and antiproliferative activity of benzo[d]isothiazole hydrazones
Several benzo[d]isothiazole hydrazones have been evaluated for their potential antiretroviral activity. Since a number of these compounds
were found to be inactive against viruses, but showed cytotoxicity at micromolar concentrations against the human CD4+ lymphocytes (MT-4)
that were used to support HIV-1 growth, they were further tested for antiproliferative activity. The compounds resulted as being cytotoxic for
MT-4 cells and new derivatives which were rationally designed and synthesized, were tested for antiproliferative activity against several leukaemia
and solid tumour cell lines. In addition, these compounds were evaluated against “normal” cell lines. Compound 2h proved to be the most
active compound and the fragment –CO−NH−N=CH−2-hydroxyphenyl was identified as being very important for biological activity, suggesting
intramolecular hydrogen bond formation or favourable mutual disposition between two important centres in the pharmacophore. 1H-NMR spectra
have been explained with the support of a conformational analysis
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