Apurinic/apyrimidinic (AP) endonuclease (APE1) is a multi-faceted protein with an essential role in the base excision repair (BER) pathway. Its implication in tumor development, progression and resistance has been confirmed in multiple cancers making it a viable target of intense investigation. Here we have designed and synthesized different classes of small molecule inhibitors of APE1’s catalytic endonuclease function containing a 3-carbamoylbenzoic scaffold. Further structural modifications have been made with the aim of increasing activity and cytotoxicity of these inhibitors. Several of our compounds exhibited low micro-molar potencies towards inhibiting APE1’s catalytic endonuclease function in vitro and thus represent novel classes of APE1 inhibitors worthy of further development

Design and Synthesis of 3-Carbamoylbenzoic Derivatives as Inhibitors of Human Apurinic/Apyrimidinic Endonuclease 1 (APE1)

AIELLO, Francesca
;
Grande F;GAROFALO, Antonio;
2012

Abstract

Apurinic/apyrimidinic (AP) endonuclease (APE1) is a multi-faceted protein with an essential role in the base excision repair (BER) pathway. Its implication in tumor development, progression and resistance has been confirmed in multiple cancers making it a viable target of intense investigation. Here we have designed and synthesized different classes of small molecule inhibitors of APE1’s catalytic endonuclease function containing a 3-carbamoylbenzoic scaffold. Further structural modifications have been made with the aim of increasing activity and cytotoxicity of these inhibitors. Several of our compounds exhibited low micro-molar potencies towards inhibiting APE1’s catalytic endonuclease function in vitro and thus represent novel classes of APE1 inhibitors worthy of further development
BER ; anticancer agents
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.11770/143394
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