Please use this identifier to cite or link to this item: https://doi.org/10.1016/j.bmc.2009.11.065
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
Source: 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. https://doi.org/10.1016/j.bmc.2009.11.065
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
URI: http://scholarbank.nus.edu.sg/handle/10635/88546
ISSN: 09680896
DOI: 10.1016/j.bmc.2009.11.065
Appears in Collections:Staff Publications

Show full item record
Files in This Item:
There are no files associated with this item.

SCOPUSTM   
Citations

9
checked on Apr 3, 2018

WEB OF SCIENCETM
Citations

6
checked on Apr 3, 2018

Page view(s)

34
checked on Apr 20, 2018

Google ScholarTM

Check

Altmetric


Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.