Nonclassical antifolates, part 3: synthesis, biological evaluation and molecular modeling study of some new 2-heteroarylthio-quinazolin-4-ones.

@article{AlOmary2013NonclassicalAP,
  title={Nonclassical antifolates, part 3: synthesis, biological evaluation and molecular modeling study of some new 2-heteroarylthio-quinazolin-4-ones.},
  author={Fatmah A. M. Al-Omary and Ghada S Hassan and S. El-Messery and M. Nagi and E. E. Habib and H. El-Subbagh},
  journal={European journal of medicinal chemistry},
  year={2013},
  volume={63},
  pages={
          33-45
        }
}
A new series of 2-heteroarylthio-6-substituted-quinazolin-4-one analogs was designed, synthesized, and evaluated for their in vitro DHFR inhibition, antimicrobial, and antitumor activities. Compounds 21, 25, and 39 proved to be active DHFR inhibitors with IC50 range of 0.3-0.8 μM. Compounds 25, 28, 33, 35 and 36 showed broad spectrum antimicrobial activity comparable to the known antibiotic gentamicin. Compound 29 showed broad spectrum antitumor activity toward several tumor cell lines with GI… Expand
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