Synthesis, biological evaluation and molecular modeling study of some new methoxylated 2-benzylthio-quinazoline-4(3H)-ones as nonclassical antifolates.

@article{ElMessery2016SynthesisBE,
  title={Synthesis, biological evaluation and molecular modeling study of some new methoxylated 2-benzylthio-quinazoline-4(3H)-ones as nonclassical antifolates.},
  author={S. El-Messery and G. S. Hassan and M. Nagi and Elsayed E. Habib and Sarah T A Al-Rashood and H. El-Subbagh},
  journal={Bioorganic & medicinal chemistry letters},
  year={2016},
  volume={26 19},
  pages={
          4815-4823
        }
}
  • S. El-Messery, G. S. Hassan, +3 authors H. El-Subbagh
  • Published 2016
  • Chemistry, Medicine
  • Bioorganic & medicinal chemistry letters
  • A new series of 2,3,6-substituted-quinazolin-4-ones was designed, synthesized, and evaluated for their in vitro DHFR inhibition, antimicrobial, and antitumor activities. Compounds 28 and 61 proved to be active DHFR inhibitors with IC50 0.02 and 0.01μM, respectively. Molecular modeling studies concluded that recognition with the key amino acid Phe34 is essential for binding and hence DHFR inhibition. Compounds 34, 56 and 66 showed broad spectrum antimicrobial activity comparable to Gentamicin… CONTINUE READING
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