Search results for "1H-Indazole-1-carboxamide"

showing 4 items of 4 documents

SYNTHESIS AND ANTIPROLIFERATIVE ACTIVITY OF 3-AMINO-N-PHENYL-1H-INDAZOLE-1-CARBOXAMIDES

2010

Recently our research group has reported the synthesis of some 3-amino-N-phenyl-1H-indazole-1-carboxamides able to inhibit at low micromolar concentrations the cell growth of many neoplastic cell lines. The above compounds are unsubstituted in the indazole nucleus and this gives the hope to obtain more active compounds if appropriate substituents are beared by the above nucleus. So, several new N-phenyl-1H-indazole-1-carboxamides 1c-h and 4l,m were prepared by reacting phenyl isocyanates 3a,b with 3-amino-1H-indazoles 2c,e,g, or 1H-indazole 2l respectively. Chemical trasformations of compounds 1a,b and 1g,h gave 3-acetamido-N-phenyl-1H-indazole-1-carboxamides 5a,b, and 3,5-diamino-N-phenyl-…

3-amino-N-phenyl-1H-indazole-1-carboxamides antiproliferative activitySettore CHIM/08 - Chimica Farmaceutica
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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…

IndazolesAntineoplastic AgentsCrystallography X-RayRetinoblastoma Proteinchemistry.chemical_compoundStructure-Activity RelationshipCell Line TumorNeoplasmsDrug DiscoverymedicineHumansCell ProliferationG0-G1 arrestPharmacologyIndazoleMolecular StructureChemistryCell growthMelanomaOrganic ChemistryCell CycleCancer1H-Indazole-1-carboxamides; Crystallographic study; G0-G1 arrest; pRb1H-Indazole-1-carboxamideGeneral MedicineCell cyclemedicine.diseaseAmidesSettore CHIM/08 - Chimica FarmaceuticaIn vitroCrystallographyc studyLeukemiapRbBiochemistryNeoplastic cell
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Synthesis of substituted 3-amino-N-phenyl-1H-indazole-1-carboxamides endowed with antiproliferative activity

2010

Abstract Several new N-phenyl-1H-indazole-1-carboxamides 1c–h and 4l,m were prepared by reacting phenyl isocyanate derivatives 3a,b with 3-amino-1H-indazole derivatives 2c,e,g or 1H-indazole 2l respectively. Chemical transformations of compounds 1a,b and 1g,h gave 3-acetamido-N-phenyl-1H-indazole-1-carboxamide derivatives 5a,b, and 3,5-diamino-N-phenyl-1H-indazole-1-carboxamide derivatives 4i, j respectively. Finally, 3,5-diacetamido-N-phenyl-1H-indazole-1-carboxamide derivatives 6a,b were prepared by acetylation of 4i, j. Some of synthesized compounds were evaluated for their in vitro antiproliferative activity against the full NCI tumor cell lines panel derived from nine clinically isolat…

IndazolesStereochemistryCellAntineoplastic AgentsRetinoblastoma Proteinchemistry.chemical_compoundCell Line TumorDrug DiscoveryG0–G1 arrestmedicineHumansCell ProliferationPharmacologyIndazoleCell growth3-amino-N-phenyl-1H-indazole-1-carboxamideMelanomaCell CycleOrganic ChemistryAntiproliferative agentsCancerGeneral Medicinemedicine.diseaseSettore CHIM/08 - Chimica FarmaceuticaIn vitropRbmedicine.anatomical_structurechemistryAcetylationK562 cellsEuropean Journal of Medicinal Chemistry
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CCDC 644638: Experimental Crystal Structure Determination

2009

Related Article: D.Raffa, B.Maggio, S.Cascioferro, M.V.Raimondi, D.Schillaci, G.Gallo, G.Daidone, S.Plescia, F.Meneghetti, G.Bombieri, A.Di Cristina, R.M.Pipitone, S.Grimaudo, M.Tolomeo|2009|Eur.J.Med.Chem.|44|165|doi:10.1016/j.ejmech.2008.03.023

Space GroupCrystallographyCrystal SystemCrystal Structure3-Amino-N-(4-(benzyloxy)phenyl)-1H-indazole-1-carboxamideCell ParametersExperimental 3D Coordinates
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