Identification of biphenyl-based hybrid molecules able to decrease the intracellular level of Bcl-2 protein in Bcl-2 overexpressing leukemia cells.

J Med Chem

Authors	Daniela Pizzirani Marinella Roberti Stefania Grimaudo Antonietta Di Cristina Rosaria Pipitone Manlio Tolomeo Maurizio Recanatini
Keywords	Humans Cell Differentiation K562 Cells Antineoplastic Agents Apoptosis HL-60 Cells Structure-Activity Relationship Ketones Spiro Compounds Biphenyl Compounds Leukemia, Myelogenous, Chronic, BCR-ABL Positive Proto-Oncogene Proteins c-bcl-2 Terphenyl Compounds
Abstract	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.
Year of Publication	2009
Journal	J Med Chem
Volume	52
Issue	21
Pages	6936-40
Date Published	2009 Nov 12
ISSN	1520-4804
URL
DOI	10.1021/jm900907s
PubMed ID	19764793
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