Ability of carbazole salts, inhibitors of Alzheimer β-amyloid fibril formation, to cross cellular membranes

Endothelin-1 Reduces P-Glycoprotein Transport Activity in an In Vitro Model of Human Adult Blood–brain Barrier

“…The modulation of Pgp activity at the human BBB is of great interest as this transporter limits the entry of a large spectrum of therapeutical drugs (Rautio et al 2006). Among Pgp substrates are some drugs used against Parkinson's disease (Uhr et al 2005), AIDS (Polli et al 1999), amyotrophic lateral sclerosis (Milane et al 2007) or Alzheimer's disease (Saengkhae et al 2007). However, this Pgp activity lowering can also counteract a natural brain defence as shown in the case of Alzheimer's disease, for instance, where Pgp has an influence on limiting amyloid-b brain accumulation (Cirrito et al 2005).…”

Biological potential of carbazole derivatives

“…10) [41]. Compound 21a known as CT is able in vitro to cross cell membranes and to penetrate rapidly inside the cells (it does not accumulate inside the mitochondria, but binds to DNA in the nucleus).…”

Carbazole ligands as c-myc G-quadruplex binders

“…Carbazole derivative 1 was synthesized following the published procedure with some modifications [76,77]. Carbazole derivatives 2 and 3 were synthesized by the method reported in our previous paper [78].…”

“…4, S2) have not reached saturation in the investigated concentration range of G4 DNA, which hampered application of Scatchard model. Instead, we used the Benesi-Hildebrand (B-H) method to estimate binding affinities of investigated ligands [76]. In this case, K b values can only be estimated with the assumption that stoichiometry of formed ligand/G4 complex is 1:1.…”