First synthesized in 2004 by the group of Peter G. Schultz [1], reversine is a 2,6-diamino substituted purine showing a potent inhibition on Aurora B, a protein kinase overexpressed in a variety of solid tumors. Due to its relevance in the cell cycle regulation, Aurora B represents a good target for anti-cancer drug development, so that reversine can be used as a promising lead compound for new potential antitumor agents[2]. Recently we have designed a series of reversine analogs by docking calculation having Aurora B kinase as specific target (Figure 1). The synthesis of new selected molecules bearing structural modifications in 2 and 6 positions has been carried out, focusing on the improvement of both the synthetic strategy (also using microwave-assisted reactions) and the products purification. The presence of different tautomeric forms for each analog is also under investigation.

Design and synthesis of reversine-like molecules as Aurora B kinase inhibitors

Sighel, Denise;Bosco, Bartolomeo;Defant, Andrea;Casarosa, Simona;Mancini, Ines
2015

Abstract

First synthesized in 2004 by the group of Peter G. Schultz [1], reversine is a 2,6-diamino substituted purine showing a potent inhibition on Aurora B, a protein kinase overexpressed in a variety of solid tumors. Due to its relevance in the cell cycle regulation, Aurora B represents a good target for anti-cancer drug development, so that reversine can be used as a promising lead compound for new potential antitumor agents[2]. Recently we have designed a series of reversine analogs by docking calculation having Aurora B kinase as specific target (Figure 1). The synthesis of new selected molecules bearing structural modifications in 2 and 6 positions has been carried out, focusing on the improvement of both the synthetic strategy (also using microwave-assisted reactions) and the products purification. The presence of different tautomeric forms for each analog is also under investigation.
Proceeding of the XV Sigma -Aldrich Young Chemists Symposium ( SAYCS 2015)
Bella F.; Spinelli D.
Roma
Società Chimica Italiana
978-88-86208-94-9
Sighel, Denise; Bosco, Bartolomeo; Defant, Andrea; Casarosa, Simona; Mancini, Ines
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11572/116028
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