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Iodine for vegetable production and livestock breeding
Published in Tatsuo Kaiho, Iodine Made Simple, 2017
Another agent for powdery mildew is called Quinoxyfen, but its mechanism differs from that of Proquinazid. Quinoxyfen inhibits the function of GTP-binding proteins in intracellular transduction. Currently, the substitution effect of pyridopyrimidine in the development of Proquinazid is presently being examined in detail. Reactivity with 7-iodine, a bromine substitute was high, but was significantly low with the three-dimensionally and electronically similar methyl group, trifluoromethyl group, phenyl group, nitro group, and cyano group. Quinozolinone derivative showed a similar tendency, and when iodine was introduced to the 6- or 6- and 8-positions, the highest level of activity was attained.
Anticancer evaluation and molecular modeling of multi-targeted kinase inhibitors based pyrido[2,3-d]pyrimidine scaffold
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2018
Heba S. A. Elzahabi, Eman S. Nossier, Nagy M. Khalifa, Rania A. Alasfoury, May A. El-Manawaty
Regarding the PC-3 cell line, hydrazino precursor 4d and pyrazolyl analogue 5a were more potent than doxorubicin as a reference standard (IC505.47 μM, 6.6 μM, and 6.8 μM respectively). Also, pyrazolyl analogue 6d as well as the hydrazone derivative 8a displayed remarkable activity of IC50 7.9 μM and 7.97 μM respectively. On the other hand, pyridopyrimidine derivatives 3a, 4b, 8 b–d exhibited moderate activity with IC50 ranged from 9.2 μM to 12 μM. Interestingly, IC90 showed promising anti-prostate cancer activity for pyrazolyl analogue 5a versus doxorubicin (IC90 14.1 μM and 13.8 μM, respectively). The rest of the test compounds showed IC90 ranged from moderate to poor activity compared to doxorubicin (Table 2).
In silico study combining QSAR, docking and molecular dynamics simulation on 2,4-disubstituted pyridopyrimidine derivatives
Published in Journal of Receptors and Signal Transduction, 2019
Maryam Tadayon, Zahra Garkani-Nejad
The dataset, including 46 molecules of pyridopyrimidine derivatives with inhibitory activity IC50 [μM] was obtained from the literature [17]. The reported IC50 values were converted to the pIC50. The structure of studied compounds was shown in Table 1.