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J Med Chem DOI:10.1021/jm900907s

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

Publication TypeJournal Article
Year of Publication2009
AuthorsPizzirani, D, Roberti, M, Grimaudo, S, Di Cristina, A, Pipitone, RMaria, Tolomeo, M, Recanatini, M
JournalJ Med Chem
Date Published2009 Nov 12
KeywordsAntineoplastic Agents, Apoptosis, Biphenyl Compounds, Cell Differentiation, HL-60 Cells, Humans, K562 Cells, Ketones, Leukemia, Myelogenous, Chronic, BCR-ABL Positive, Proto-Oncogene Proteins c-bcl-2, Spiro Compounds, Structure-Activity Relationship, Terphenyl Compounds

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.


Alternate JournalJ. Med. Chem.
PubMed ID19764793