A novel class of highly potent multidrug resistance reversal agents: Disubstituted adamantyl derivatives

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Title
A novel class of highly potent multidrug resistance reversal agents: Disubstituted adamantyl derivatives
Author(s)
K H Min; Y Xia; E K Kim; Y Jin; N Kaur; E S Kim; D K Kim; H Y Jung; Y Choi; M K Park; Y K Min; Kiho Lee; Kyeong Lee
Bibliographic Citation
Bioorganic & Medicinal Chemistry Letters, vol. 19, no. 18, pp. 5376-5379
Publication Year
2009
Abstract
Novel disubstituted adamantyl derivatives were synthesized and evaluated in a P-glycoprotein dependent multidrug resistance cancer cell line. The hit to lead optimization provided potent MDR reversal agents. Some potent adamantyl derivatives were more than 10-fold more potent than verapamil without considerable intrinsic cytotoxicity. The 3-trifluorophenyl derivative 14f did not affect the metabolism of CYP450 3A4, whereas most of MDR revertants had a weak inhibitory effect.
Keyword
ABC transporterAdamantaneCYP3A4MES-SA/DX5Multidrug resistanceP-glycoprotein
ISSN
0960-894X
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/j.bmcl.2009.07.127
Type
Article
Appears in Collections:
1. Journal Articles > Journal Articles
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