Synthesis, biological evaluation and molecular modeling study of 2-(1,3,4-thiadiazolyl-thio and 4-methyl-thiazolyl-thio)-quinazolin-4-ones as a new class of DHFR inhibitors.

@article{AlRashood2014SynthesisBE,
  title={Synthesis, biological evaluation and molecular modeling study of 2-(1,3,4-thiadiazolyl-thio and 4-methyl-thiazolyl-thio)-quinazolin-4-ones as a new class of DHFR inhibitors.},
  author={Sarah T A Al-Rashood and G. S. Hassan and S. El-Messery and M. Nagi and El-Sayed E. Habib and Fatmah A. M. Al-Omary and H. El-Subbagh},
  journal={Bioorganic & medicinal chemistry letters},
  year={2014},
  volume={24 18},
  pages={
          4557-4567
        }
}
  • Sarah T A Al-Rashood, G. S. Hassan, +4 authors H. El-Subbagh
  • Published 2014
  • Chemistry, Medicine
  • Bioorganic & medicinal chemistry letters
  • A new series of 2-(1,3,4-thiadiazolyl- or 4-methyl-thiazolyl)thio-6-substituted-quinazolin-4-one analogs was designed, synthesized, and evaluated for their in vitro DHFR inhibition, antimicrobial, and antitumor activities. Compounds 29, 34, and 39 proved to be the most active DHFR inhibitors with IC50 values range of 0.1-0.6 μM. Compounds 28, 31 and 33 showed remarkable broad-spectrum antimicrobial activity comparable to the known antibiotic Gentamicin. Compounds 26, 33, 39, 43, 44, 50, 55 and… CONTINUE READING
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