Nonclassical antifolates, part 5. Benzodiazepine analogs as a new class of DHFR inhibitors: synthesis, antitumor testing and molecular modeling study.

@article{ElSubbagh2014NonclassicalAP,
  title={Nonclassical antifolates, part 5. Benzodiazepine analogs as a new class of DHFR inhibitors: synthesis, antitumor testing and molecular modeling study.},
  author={H. El-Subbagh and G. S. Hassan and S. El-Messery and Sarah T A Al-Rashood and Fatmah A. M. Al-Omary and Y. S. Abulfadl and M. Shabayek},
  journal={European journal of medicinal chemistry},
  year={2014},
  volume={74},
  pages={
          234-45
        }
}
  • H. El-Subbagh, G. S. Hassan, +4 authors M. Shabayek
  • Published 2014
  • Chemistry, Medicine
  • European journal of medicinal chemistry
  • A new series of tetrahydro-quinazoline and tetrahydro-1H-dibenzo[b,e][1,4]diazepine analogs were synthesized and tested for their DHFR inhibition and in vitro antitumor activity. Compound 35 showed a remarkable DHFR inhibitory potency (IC₅₀, 0.004 μM) which is twenty fold more active than methotrexate (MTX). Compounds 17 and 23 proved to be fifteen fold more active than the known antitumor 5-FU, with MG-MID GI₅₀, TGI, and LC₅₀ values of 1.5, 46.8, 93.3 and 1.4, 17.4, 93.3 μM, respectively… CONTINUE READING
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