Search results for " G0-G1"
showing 3 items of 3 documents
Synthesis and antiproliferative activity of 3-amino-N-phenyl-1H-indazole-1-carboxamides
2007
Abstract A series of new 3-amino-N-phenyl-1H-indazole-1-carboxamides 10 have been prepared from commercially available phenyl isocyanate precursors 8 and 3-aminoindazole 9. Some of the synthesized compounds were evaluated for their in vitro antineoplastic activity against 60 human cell lines derived from seven clinically isolated cancer types (lung, colon, melanoma, renal, ovarian, brain, and leukemia) according to the NCI standard protocol. The test results indicated that 3-amino-1H-indazole-1-carboxamides 10 were endowed with an interesting antiproliferative activity. The most active compounds of this series, 10d,e, were able to inhibit cell growth of many neoplastic cell lines at concent…
Synthesis and antiproliferative activity of new derivatives containing the polycyclic system 5,7:7,13-dimethanopyrazolo[3,4-b]pyrazolo[3’,4’:2,3]azep…
2013
The reaction under reflux between 1-phenyl-3-R-5-methylaminopyrazoles and 2,5-hexanedione lead to 5,7:7,13-dimethanopyrazolo[3,4-b]pyrazolo[3′,4′:2,3]azepino[4,5-f]azocine derivatives 3b–g. These unusual molecules show the structural complexity of many biologically active natural products and are endowed with the chemical diversity that is required in drug discovery. The compounds 3b,e were reduced by hydrogen in the presence of Palladium on activated charcoal to give the dihydro derivatives 5b,e. Compounds 3b–f and 5b,e were selected by the NCI to evaluate their in vitro antiproliferative activity against 60 human cell lines derived from nine clinically isolated cancer types (leukaemia, lu…
Synthesis and antiproliferative activities of two new analogs of tetrazepinones
Based on the encouraging results, we report the multistep synthesis and the biologicalo results of two new analogs of tetrazepinones: the 3,5-dimethyl-6-phenyl-8-(trifluoromethyl-5,6-dihydropyrazo1o[3-4-f]1,2,35)tetrazepin-4(3H)-one and the 3-(2-chloroethyl)-5-methyl-6-phenyl-8-(trifluoromethyl-5,6-dihydropyrazo1o[3-4-f]1,2,35)tetrazepin-4(3H)-one. Both compounds showed a pro-apoptotic activity against HL60 and K562 resistant cell lines. Flow cytometry studies carried out 0n K562 cells allowed to establish that the methyl derivative induces G0-G1, phase arrest followed by apoptosis, whereas the chloroethyl derivative is a not phase-specific agent.