Synthesis, dihydrofolate reductase inhibition, antitumor testing, and molecular modeling study of some new 4(3H)-quinazolinone analogs.
@article{AlRashood2006SynthesisDR, title={Synthesis, dihydrofolate reductase inhibition, antitumor testing, and molecular modeling study of some new 4(3H)-quinazolinone analogs.}, author={Sarah T A Al-Rashood and Ihsan A Aboldahab and M. Nagi and L. Abou-zeid and A. Abdel-Aziz and S. G. Abdel-hamide and K. Youssef and A. M. Al-Obaid and H. El-Subbagh}, journal={Bioorganic & medicinal chemistry}, year={2006}, volume={14 24}, pages={ 8608-21 } }
In order to produce potent new leads for anticancer drugs, a new series of quinazoline analogs was designed to resemble methotrexate (MTX, 1) structure features and fitted with functional groups believed to enhance inhibition of mammalian DHFR activity. Molecular modeling studies were used to assess the fit of these compounds within the active site of human DHFR. The synthesized compounds were evaluated for their ability to inhibit mammalian DHFR in vitro and for their antitumor activity in a… CONTINUE READING
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