1474030-57-3Relevant academic research and scientific papers
4-Arylamino-6-nitroquinazolines: Synthesis and their activities against neglected disease leishmaniasis
Saad, Syed Muhammad,Ghouri, Nida,Perveen, Shahnaz,Khan, Khalid Mohammed,Choudhary, M. Iqbal
, p. 13 - 20 (2015/12/05)
4-Arylamino-6-nitroquinazolines (2-25) were synthesized and evaluated for their leishmanicidal activities against Leishmania major promastigotes in vitro with IC50 values Combining double low line 1.87-61.48 μM. Among the twenty four synthetic derivatives, 4-[4′-(methylsulfanyl)phenyl]amino-6-nitroquinazoline (21), and 4-(2′-methoxyphenyl)amino-6-nitroquinazoline (8) showed excellent antileishmanial activities with IC50 values 1.87 ± 0.31 and 4.37 ± 0.02 μM, respectively, more active than the standard drug, pentamidine (IC50 Combining double low line 5.09 ± 0.09 μM). Compound 16 (IC50 Combining double low line 6.53 ± 0.21 μM) displayed an activity comparable to the standard. Compounds 15 (IC50 Combining double low line 9.04 ± 0.03 μM), 18 (IC50 Combining double low line 12.28 ± 0.18 μM), 14 (IC50 Combining double low line 19.87 ± 0.22 μM), and 5 (IC50 Combining double low line 24.03 ± 2.71 μM) also showed good activities.
Quinazoline and tetrahydropyridothieno[2,3-d]pyrimidine derivatives as irreversible EGFR tyrosine kinase inhibitors: Influence of the position 4 substituent
Hamed, Mostafa M.,Abou El Ella, Dalal A.,Keeton, Adam B.,Piazza, Gary A.,Engel, Matthias,Hartmann, Rolf W.,Abadi, Ashraf H.
, p. 1202 - 1207 (2013/08/23)
Herein, we describe new quinazoline and tetrahydropyridothieno[2,3-d] pyrimidine derivatives with an acrylamido group at positions 6 and 7 respectively, and with variable anilino, sulfonamido and cycloalkylamino substituents at position 4. The lipophilic and steric properties of the position 4 substituent seem crucial for activity. Several compounds were more active than gefitinib in inhibiting the wild type EGFR enzyme, the autophosphorylation of the mutant EGFR expressing cell line (H1975), and the growth of cell lines with wild type and mutant EGFR tyrosine kinase. Moreover, a novel synthesis of the quinazoline nucleus from a formimidate derivative is described.
