Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 26, Issue 10, Pages 2450-2454Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.03.108
Keywords
Diazaphosphinanes; Coumarin; Lawesson's reagent; Cytotoxic activity; Anti-tyrosinase activity
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Funding
- Ministry of Higher Education and Scientific Research of Tunisia
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A series of alpha-aminocarbonitriles 2a-h, obtained by a condensation reaction of 4-hydroxycoumarin with malononitrile and a series of arylaldehydes, was reacted with Lawesson's reagent to give the diazaphosphinanes 3a-h and 3a'-h' as diastereoisomers. All the synthesized compounds were characterized by spectroscopic means such as NMR (H-1, C-13, P-31) and MS. The synthesized compounds were evaluated for their cytotoxic activity in vitro against two tumor cell lines MCF-7 and HCT-116 and for their anti-tyrosinase effect. The results showed a moderate cytotoxic activity for most compounds and nearly all tested derivatives have been found considerable tyrosinase inhibitors. (C) 2016 Elsevier Ltd. All rights reserved.
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