Non-classical antifolates. Part 2: synthesis, biological evaluation, and molecular modeling study of some new 2,6-substituted-quinazolin-4-ones.

@article{AlOmary2010NonclassicalAP,
  title={Non-classical antifolates. Part 2: synthesis, biological evaluation, and molecular modeling study of some new 2,6-substituted-quinazolin-4-ones.},
  author={Fatmah A. M. Al-Omary and Laila A. Abou-zeid and Mahmoud N. Nagi and E E Habib and Alaa A-M Abdel-Aziz and Adel S El-Azab and Sami G. Abdel-Hamide and Mohamed A Al-Omar and Abdulrahman M. Al-Obaid and Hussein Ibrahim El-Subbagh},
  journal={Bioorganic & medicinal chemistry},
  year={2010},
  volume={18 8},
  pages={2849-63}
}
A new series of 2,6-substituted-quinazolin-4-ones was designed, synthesized, and evaluated for their in vitro DHFR inhibition, antimicrobial, and antitumor activities. Compounds 22, 33-37, 39-43, and 45 proved to be active DHFR inhibitors with IC(50) range of 0.4-1.0microM. Compound 18 showed broad-spectrum antimicrobial activity comparable to the known antibiotic gentamicin. Compounds 34 and 36 showed antitumor activity at GI(50) (MG-MID) concentrations of 11.2, and 24.2microM, respectively… CONTINUE READING

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