Antiproliferative activity against MCF-7 breast cancer cells by diamino-triazaspirodiene antifolates

Abstract

Two triazaspirodienes, having similar phenoxy propyloxy side chain, were identified as potent mammalian dihydrofolate reductase inhibitors; one having a 6,5-spiro bicyclic ring system (IC50 = 2.3 nm) and the other a 6,6-spiro bicyclic system (IC50 = 6.9 nm). They also showed more than 50% antiproliferative activity against the MCF-7 breast cancer cells at 20 μm. This study demonstrated the potential lead of the diamino- triazaspirodienes in anticancer chemotherapeutical agents' discovery. © 2009 John Wiley & Sons A/S.