| Literature DB >> 19679475 |
Kyung Hoon Min1, Yan Xia, Eun Kyung Kim, Yinglan Jin, Navneet Kaur, Eun Seon Kim, Dae Kyong Kim, Hwa Young Jung, Yongseok Choi, Mi-Kyung Park, Yong Ki Min, Kiho Lee, Kyeong Lee.
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.Entities:
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Year: 2009 PMID： 19679475 DOI： 10.1016/j.bmcl.2009.07.127
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823