AI Article Synopsis
- A series of fourteen quinoline-based chalcones were tested as potential inhibitors of reverse transcriptase (RT), an enzyme important for viral RNA replication.
- The results indicated that the specific types and positions of substituents on the chalcones significantly influenced their effectiveness in inhibiting RT.
- Notably, the compounds A4 and A6 exhibited strong interactions with RT, showcasing high binding affinity and low IC50 values, indicating their potential as effective inhibitors.
Article Abstract
A series of fourteen (A1 - A14) 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 A4 andA6 showed high interaction with RT, contributing high free binding energy (ΔG -9.30 and -9.13kcal) and RT inhibition value (IC50 0.10μg/ml and 0.11μg/ml).
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| http://dx.doi.org/10.1016/j.bioorg.2016.02.008 | DOI Listing |
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