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A novel class of highly potent multidrug resistance reversal agents: Disubstituted adamantyl derivatives
- Authors
- Min, Kyung Hoon; Xia, Yan; Kim, Eun Kyung; Jin, Yinglan; Kaur, Navneet; Kim, Eun Seon; Kim, Dae Kyong; Jung, Hwa Young; Choi, Yongseok; Park, Mi-Kyung; Min, Yong Ki; Lee, Kiho; Lee, Kyeong
- Issue Date
- Sep-2009
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Multidrug resistance; MES-SA/DX5; ABC transporter; P-glycoprotein; Adamantane; CYP3A4
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.19, no.18, pp 5376 - 5379
- Pages
- 4
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 19
- Number
- 18
- Start Page
- 5376
- End Page
- 5379
- ISSN
- 0960-894X
1464-3405
- 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. (C) 2009 Elsevier Ltd. All rights reserved.
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