6533b829fe1ef96bd128ad2f
RESEARCH PRODUCT
Synthesis, antiproliferative activity and possible mechanism of action of novel 2-acetamidobenzamides bearing the 2-phenoxy functionality.
Maria Grazia CusimanoStella CascioferroBenedetta MaggioGabriella CancemiErnest HamelFabiana PlesciaMaria Valeria RaimondiAntonella D’anneoRuoli BaiGiuseppe DaidoneDemetrio RaffaMarianna Lauricellasubject
3003Clinical BiochemistryCellPharmaceutical ScienceAntineoplastic AgentsApoptosisAntiproliferative activityPharmacologyG0/G1 arrestBiochemistryArticle2-(2-Phenoxyacetamido)benzamideAntineoplastic AgentStructure-Activity RelationshipBenzamideSettore BIO/10 - BiochimicaCell Line TumorDrug DiscoveryG1 Phase Cell Cycle CheckpointK562 CellmedicineHumansMolecular BiologyCell ProliferationCell growthChemistryDrug Discovery3003 Pharmaceutical ScienceOrganic ChemistryApoptosiCell cyclemedicine.diseaseCaspaseSettore CHIM/08 - Chimica FarmaceuticaG1 Phase Cell Cycle CheckpointsLeukemiamedicine.anatomical_structureMicroscopy FluorescenceCell cultureApoptosisCaspasesBenzamidesMolecular MedicineDrug Screening Assays AntitumorK562 CellsPro-caspase 3HumanK562 cellsChronic myelogenous leukemiadescription
Several new 2-(2-phenoxyacetamido)benzamides 17a-v, 21 and 22 were synthesized by stirring in pyridine the acid chlorides 16a-e and the appropriate5-R-4-R1-2-aminobenzamide 15a-e and initially evaluated in vitro for antiproliferative activity against the K562 (human chronic myelogenous leukemia) cell line. Some of synthesized compounds were evaluated for their in vitro antiproliferative activity against the full NCI tumor cell line panel derived from nine clinically isolated cancer types (leukemia, non-small cell lung, colon, CNS, melanoma, ovarian, renal, prostate and breast). The most active compounds caused an arrest of K562 cells in the G0-G1 phase of cell cycle and induction of apoptosis, which was mediated by caspase activation.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2015-07-01 | Bioorganicmedicinal chemistry |