- Synthesis of potent BCRP inhibitor-Ko143
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Two routes for the synthesis of potent BCRP inhibitor-Ko143 are reported. The key intermediate, 6-methoxytryptophan derivative, was synthesized by an improved procedure, ytterbium triflate-promoted coupling between 6-methoxyindole and optically active 1-b
- Li, Yuexian,Hayman, Erik,Plesescu, Mihaela,Prakash, Shimoga R.
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- Synthesis of a new inhibitor of breast cancer resistance protein with significantly improved pharmacokinetic profiles
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The design, synthesis, in vitro inhibitory potency, and pharmacokinetic (PK) profiles of Ko143 analogs are described. Compared to commonly used Ko143, the new breast cancer resistance protein (BCRP) inhibitor (compound A) showed the same potency and a sig
- Li, Yuexian,Woo, Jiyeon,Chmielecki, Jessica,Xia, Cindy Q.,Liao, Mingxiang,Chuang, Bei-Ching,Yang, Johnny J.,Guan, Miao Y.,Plesescu, Mihaela,Prakash, Shimoga R.
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- INHIBITOR OF BREAST CANCER RESISTANCE PROTEIN (BCRP)
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Disclosed are compounds that inhibit breast cancer resistance protein (BCRP), of which compound (I-1), ((3S, 6S, 12aS)-6-isobutyl-9-methoxy-3-methyl-2,3,6,7, 12, 12a- hexahydropyrazino[1',2': 1,6]pyrido[3,4-b]indole-1,4-dione) or a pharmaceutically accept
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Paragraph 00109
(2015/04/28)
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