Thiazolo[4,5-d]pyridazine analogues as a new class of dihydrofolate reductase (DHFR) inhibitors: Synthesis, biological evaluation and molecular modeling study.

@article{Ewida2017Thiazolo45dpyridazineAA,
  title={Thiazolo[4,5-d]pyridazine analogues as a new class of dihydrofolate reductase (DHFR) inhibitors: Synthesis, biological evaluation and molecular modeling study.},
  author={Menna A Ewida and D. A. Abou El Ella and Deena S. Lasheen and Heba A Ewida and Yomna I El-Gazzar and H. El-Subbagh},
  journal={Bioorganic chemistry},
  year={2017},
  volume={74},
  pages={
          228-237
        }
}
A new series of 1,3-thiazoles and thiazolo[4,5-d]pyridazine both bearing the 2-thioureido function were designed, synthesized and evaluated for their invitro DHFR inhibition and antitumor activities. Compound 26 proved to be the most active DHFR inhibitor (IC50 of 0.06μM). Compound 4, 20 and 21 showed in vitro antitumor activity against a collection of cancer cell lines. Compound 26 proved lethal to HS 578T breast cancer cell line with IC50 value of 0.8μM, inducing cell cycle arrest and… Expand
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