- DEUTERATED ANALOGS OF ELACRIDAR
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The present invention relates to efflux inhibitor compounds, compositions, and methods of using the same. More specifically, the instant invention comprises deuterated analogs of elacridar with superior pharmacokinetic properties such that it is now possi
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Paragraph 0028; 00180-00181
(2019/10/15)
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- Synthesis of new acridone derivatives, inhibitors of NS3 helicase, which efficiently and specifically inhibit subgenomic HCV replication
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A new goup of acridone derivatives, obtained by reaction of acridone-4-carboxylic acid derivatives with aromatic amines, was tested to determine the inhibitory properties toward the NS3 helicase of hepatitis C virus (HCV). Six compounds inhibited the NS3 helicase at low concentrations (IC 50 from 1.5 to 20 μM). The acridone derivatives probably act via intercalation into double-stranded nucleic acids with a strong specificity for double-stranded RNA, although an interaction with the enzyme cannot be excluded. Testing in the subgenomic HCV replicon system revealed that compounds 10 and 13 are efficient RNA replication inhibitors, with EC50 of 3.5 and 1 μM and therapeutic indexes of >28 and 20, respectively. Compound 16, with EC50 1000, is extremely specific and practically noncytotoxic at the concentrations tested, proving that the acridone derivatives may be regarded as potential antiviral agents. Although the mechanism of action of 16 in the replicon system remains unclear, it is the key lead compound for further development of anti-HCV drugs.
- Stankiewicz-Drogoń, Anna,D?rner, Bernd,Erker, Thomas,Boguszewska-Chachulska, Anna M.
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scheme or table
p. 3117 - 3126
(2010/09/18)
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- Synthesis and small-animal positron emission tomography evaluation of [11C]-elacridar as a radiotracer to assess the distribution of P-glycoprotein at the blood-brain barrier
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With the aim to develop a positron emission tomography (PET) tracer to assess the distribution of P-glycoprotein (P-gp) at the blood-brain barrier (BBB) in vivo, the potent third-generation P-gp inhibitor elacridar (1) was labeled with 11C by r
- D?rner, Bernd,Kuntner, Claudia,Bankstahl, Jens P.,Bankstahl, Marion,Stanek, Johann,Wanek, Thomas,Stundner, Gloria,Mairinger, Severin,L?scher, Wolfgang,Müller, Markus,Langer, Oliver,Erker, Thomas
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supporting information; experimental part
p. 6073 - 6082
(2010/03/24)
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- Potential antitumor agents. 40. Orally active 4,5-disubstituted derivatives of amsacrine
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The DNA-intercalating agent amsacrine is an effective drug for the treatment of human leukemias and lymphomas but has minimal solid tumor activity. As a first step in identifying analogues with a wider spectrum of activity, a comparison was made of the in
- Denny,Atwell,Baguley
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p. 363 - 367
(2007/10/02)
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