An efficient acid catalyzed methodology has been employed to synthesize a variety of aza-flavanones and their α-glucosidase inhibitory activity is evaluated using acarbose, miglitol and voglibose as reference standards. Molecular modeling studies were performed for all compounds to identify the important binding modes responsible for the inhibition activity of α-glucosidase which helped find key interactions between the enzyme and the active compounds. Among all the compounds , and have shown high α-glucosidase inhibition activity compared to standard reference drugs and have been identified as promising potential antidiabetic agents. This study is the first biological evaluation of aza-flavanones as α-glucosidase inhibitors.
Background:
In the present study, new triazine derivatives 3, 4, 5, 6, 8 and 10 were
synthesized starting from readily available cyanuric chloride 1 via nucleophilic displacement with
morpholine followed by Suzuki or Stille coupling reactions and then the thermal displacement of
chlorine atom with diverse substituted amines.
Methods:
All synthesized compounds were screened for their cytotoxic activity against HT-29,
MDA-MB-231, and HEK293 cell lines.
Results and Conclusion:
Compounds 6a (IC50 (µM): 0.32 for HT-29 and 2.92 for MDA-MB-231)
and 8c (IC50 (µM): 1.40 for HT-29 and 1.60 for MDA-MB-231) have been identified and compared
with Doxorubicin and ZSTK474 as the reference standards.
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