Nonclassical antifolates, part 4. 5-(2-aminothiazol-4-yl)-4-phenyl-4H-1,2,4-triazole-3-thiols as a new class of DHFR inhibitors: synthesis, biological evaluation and molecular modeling study.

@article{Hassan2013NonclassicalAP,
  title={Nonclassical antifolates, part 4. 5-(2-aminothiazol-4-yl)-4-phenyl-4H-1,2,4-triazole-3-thiols as a new class of DHFR inhibitors: synthesis, biological evaluation and molecular modeling study.},
  author={G. S. Hassan and S. El-Messery and Fatmah A. M. Al-Omary and Sarah T A Al-Rashood and M. Shabayek and Y. S. Abulfadl and El-Sayed E. Habib and S. El-Hallouty and Walid Fayad and K. Mohamed and B. El-Menshawi and H. El-Subbagh},
  journal={European journal of medicinal chemistry},
  year={2013},
  volume={66},
  pages={
          135-45
        }
}
  • G. S. Hassan, S. El-Messery, +9 authors H. El-Subbagh
  • Published 2013
  • Chemistry, Medicine
  • European journal of medicinal chemistry
  • A new series of compounds possessing 5-(2-aminothiazol-4-yl)-4-phenyl-4H-1,2,4-triazole-3-thiol skeleton was designed, synthesized, and evaluated for their in vitro DHFR inhibition, antimicrobial, antitumor and schistosomicidal activities. Four active compounds were allocated, the antibacterial 22 (comparable to gentamicin and ciprofloxacin), the schistosomicidal 29 (comparable to praziquantel), the DHFR inhibitor 34 (IC₅₀ 0.03 μM, 2.7 fold more active than MTX), and the antitumor 36… CONTINUE READING
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