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Title: Antifolate and antiproliferative activity of 6,8,10-triazaspiro[4.5]deca-6,8-dienes and 1,3,5-triazaspiro[5.5]undeca-1,3-dienes
Authors: Ma, X. 
Chui, W.-K. 
Keywords: 1,3,5-Triazines
Antiproliferative activity
DHFR inhibitors
Spiro rings
Issue Date: 15-Jan-2010
Citation: Ma, X., Chui, W.-K. (2010-01-15). Antifolate and antiproliferative activity of 6,8,10-triazaspiro[4.5]deca-6,8-dienes and 1,3,5-triazaspiro[5.5]undeca-1,3-dienes. Bioorganic and Medicinal Chemistry 18 (2) : 737-743. ScholarBank@NUS Repository.
Abstract: Two series of triazaspiroalkanedienes, bearing a substituted phenoxy propyloxy side chain, were identified as potent mammalian DHFR inhibitors. One series has a 6,5-spiro bicyclic ring system and the other series has a 6,6-spiro bicyclic system. Both series were synthesized and tested for in vitro mammalian DHFR inhibitory activity and antiproliferative activity against A549 human lung-cancer cells. Compound 3c showed the highest antiproliferative activity against A549 cells with an IC50 value of 27.1 nM. Rescue experiment confirmed its antifolate antiproliferative mechanism. The excellent antifolate and antiproliferative activity of selected analogues presented in this study warrants further investigation as potential leads in the anticancer drug discovery. © 2009 Elsevier Ltd. All rights reserved.
Source Title: Bioorganic and Medicinal Chemistry
ISSN: 09680896
DOI: 10.1016/j.bmc.2009.11.065
Appears in Collections:Staff Publications

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