Journal
BIOORGANIC CHEMISTRY
Volume 65, Issue -, Pages 175-182Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2016.02.008
Keywords
Quinoline; Chalcone; Theoretical; Acetophenone; RT reverse transcriptase
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A series of fourteen (A(1) - A(14)) qunioline based chalcones were screened for reverse transcriptase inhibitors (RT) and found potentially active against RT. Bioassay, theoretical and dockings studies with RT (the enzyme required for reverse transcription of viral RNA) results showed that the type and positions of the substituents seemed to be critical for their inhibition against RT. The bromo and chloro substituted chalcone displayed high degree of inhibition against RT. The A(4) andA(6) showed high interaction with RT, contributing high free binding energy (Delta G -9.30 and -9.13 kcal) and RT inhibition value (IC50 0.10 mu g/ml and 0.11 mu g/ml). (C) 2016 Elsevier Inc. All rights reserved.
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