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Title 

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

Authors 

K H MinY XiaE K KimY JinN KaurE S KimD K KimH Y JungY ChoiM K ParkY K MinKiho LeeKyeong Lee

Publisher 

Elsevier

Issue Date 

2009

Citation 

Bioorganic & Medicinal Chemistry Letters, vol. 19, no. 18, pp. 5376-5379

Keywords 

ABC transporterAdamantaneCYP3A4MES-SA/DX5Multidrug resistanceP-glycoprotein

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.

ISSN 

0960-894X

Link 

http://dx.doi.org/10.1016/j.bmcl.2009.07.127

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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