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

Bioorg Med Chem Lett. 2009 Sep 15;19(18):5376-9. doi: 10.1016/j.bmcl.2009.07.127.

Kyung Hoon Min ¹, 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

Affiliations

Affiliation

1 College of Pharmacy, Chung-Ang University, Seoul 156-756, Republic of Korea. [email protected]

PMID: 19679475 DOI: 10.1016/j.bmcl.2009.07.127

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.

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