6533b82afe1ef96bd128b87d
RESEARCH PRODUCT
Isoindolo[2,1-c]benzo[1,2,4]triazines: a new ring system with antiproliferative activity.
Gaetano DattoloAnna Maria AlmericoPatrizia DianaAntonino LauriaAnnamaria MartoranaGirolamo CirrincionePaola BarrajaAlessandra Montalbanosubject
IndolesColorectal cancerClinical BiochemistryCellPharmaceutical ScienceAntineoplastic AgentsBiochemistryStructure-Activity RelationshipBreast cancerCell Line TumorNeoplasmsDrug DiscoverymedicineHumans3D-Mind Antiproliferative activity Isoindolo-benzotriazineMolecular BiologyCell ProliferationMolecular StructureChemistryTriazinesMelanomaOrganic ChemistryCancerStereoisomerismmedicine.diseaseLeukemiamedicine.anatomical_structureCell cultureImmunologyCancer researchMolecular MedicineDrug Screening Assays AntitumorOvarian cancerdescription
Abstract A series of isoindolo-benzo-triazines of type 4 was obtained by diazotization of 2-(2-aminoaryl)-1-cyanoisoindoles 3a – j . All the synthesized derivatives were screened by the National Cancer Institute (NCI, Bethesda, USA), for in vitro antitumor activity against a 3-human cancer cell line panel consisting of MCF7 (breast), NCI-H460 (lung), and SF-268 (CNS). Derivatives 4a , f , i , j were selected to be evaluated in the full panel of about 50 human tumor cell lines derived from nine human cancer cell types and showed antiproliferative activity generally in the micromolar range. The most sensitive cell lines were: MOLT-4 and SR of the leukemia subpanel, A549/ATCC and EKVX of the nonsmall cell lung subpanel, COLO-205 of the colon cancer subpanel, LOX IMVI of the Melanoma subpanel, OVCAR-8 of the ovarian cancer subpanel, and MCF7, BT-549 of the breast cancer subpanel.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2006-05-19 | Bioorganicmedicinal chemistry |