Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 21, Issue 13, Pages 3760-3779Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.04.034
Keywords
N-Hydroxyalkyl-2-aminophenothiazines; Sulfoxide and sulfone derivatives; MDR inhibition; Buchwald-Hartwig cross-coupling reaction; Resolution of racemate
Funding
- Hungarian Scientific Research Fund [OTKA-NK77784]
- Szeged Foundation for Cancer Research
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Novel N-hydroxyalkyl-2-aminophenothiazines implying a tetrazole moiety at the alkyl chain have been synthesized by hydroboration oxidation of dienes followed by Buchwald Hartwig cross-coupling reaction. Also, some sulfoxide and sulfone derivatives have been prepared by selective oxidations. MDR inhibition studies on rat hepatocyte cell culture revealed that some derivatives exhibit marked biological efficacy exceeding that of the standard verapamil (e.g., 3h, 4h, 16). Selected derivatives were subjected to chemical resolution to provide both enantiomers which were shown of similar activity on P-gp interaction measurements. The new compounds exhibited no toxicity. (C) 2013 Elsevier Ltd. All rights reserved.
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