3-(6-isobutyl-9-methoxy-1-4-dioxo-1-2-3-4-6-7-12-12a-octahydropyrazino(1--2--1-6)pyrido(3-4-b)indol-3-yl)propionic-acid-tert-butyl-ester and estrone-sulfate

3-(6-isobutyl-9-methoxy-1-4-dioxo-1-2-3-4-6-7-12-12a-octahydropyrazino(1--2--1-6)pyrido(3-4-b)indol-3-yl)propionic-acid-tert-butyl-ester has been researched along with estrone-sulfate* in 1 studies

Other Studies

1 other study(ies) available for 3-(6-isobutyl-9-methoxy-1-4-dioxo-1-2-3-4-6-7-12-12a-octahydropyrazino(1--2--1-6)pyrido(3-4-b)indol-3-yl)propionic-acid-tert-butyl-ester and estrone-sulfate

ArticleYear
Synthesis of a new inhibitor of breast cancer resistance protein with significantly improved pharmacokinetic profiles.
    Bioorganic & medicinal chemistry letters, 2016, Jan-15, Volume: 26, Issue:2

    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 significantly improved PK profile in rats (lower clearance [1.54L/h/kg] and higher bioavailability [123%]). Ko143 on the other hand suffers from poor bioavailability. Compared to Ko143, compound A would be a useful probe for delineating the role of BCRP during in vivo studies in animals.

    Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; ATP Binding Cassette Transporter, Subfamily G, Member 2; Caco-2 Cells; Diketopiperazines; Estrone; Heterocyclic Compounds, 4 or More Rings; Humans; Rats; Stereoisomerism; Structure-Activity Relationship

2016