Synthesis, biological evaluation and molecular modeling study of new (1,2,4-triazole or 1,3,4-thiadiazole)-methylthio-derivatives of quinazolin-4(3H)-one as DHFR inhibitors.

@article{ElGazzar2017SynthesisBE,
  title={Synthesis, biological evaluation and molecular modeling study of new (1,2,4-triazole or 1,3,4-thiadiazole)-methylthio-derivatives of quinazolin-4(3H)-one as DHFR inhibitors.},
  author={Yomna I El-Gazzar and H. Georgey and S. El-Messery and Heba A Ewida and Ghada S Hassan and Marwa M. Raafat and Menna A Ewida and H. El-Subbagh},
  journal={Bioorganic chemistry},
  year={2017},
  volume={72},
  pages={
          282-292
        }
}
A new series of 2-mercapto-quinazolin-4-one analogues was designed, synthesized and evaluated for their in vitro DHFR inhibition, antitumor and antimicrobial activity. Compound 17 proved to be the most active DHFR inhibitor with IC50 value of 0.01μM, eight fold more active than methotrexate (MTX). Compounds 16 and 24 showed antitumor activity against human Caco2 colon and MCF-7 breast tumor cell lines with IC50 values of 25.4 and 9.5μg/ml, respectively. Compounds 15, 20, 21 and 30 showed… Expand
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References

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