6533b82bfe1ef96bd128cefc

RESEARCH PRODUCT

Identification of Biphenyl-Based Hybrid Molecules Able To Decrease the Intracellular Level of Bcl-2 Protein in Bcl-2 Overexpressing Leukemia Cells

Stefania GrimaudoMaria Rosaria PipitoneMaurizio RecanatiniManlio TolomeoMarinella RobertiAntonietta Di CristinaDaniela PizziraniDaniela Pizzirani

subject

Antineoplastic AgentsApoptosisHL-60 CellsChemical synthesisStructure-Activity RelationshipLeukemia Myelogenous Chronic BCR-ABL PositiveTerphenyl CompoundsDrug DiscoverymedicineHumansSpiro CompoundsChemistryBiphenyl CompoundsCell DifferentiationBiological activityKetonesmedicine.diseaseIn vitroLeukemiaProto-Oncogene Proteins c-bcl-2BiochemistryApoptosisCell cultureMolecular MedicineTerphenyl CompoundsK562 CellsIntracellular

description

With the aim of enhancing the structural complexity and diversity of an existing collection of bi- and terphenyl compounds, we synthesized hybrid molecules comprising of spirocyclic ketones (a complexity-bearing core) and bi/terphenyls (privileged fragments). Compounds 1, 3, 4, and 6 showed well-defined activity on apoptosis and differentiation, making them potential leads for development as new anticancer agents and chemical probes to study signaling networks in neoplastic cells.

yearjournalcountryeditionlanguage
2009-09-18Journal of Medicinal Chemistry
https://doi.org/10.1021/jm900907s