Synthesis and biological evaluation of novel 4-(hetero) aryl-2-piperazino quinazolines as anti-leishmanial and anti-proliferative agents

Antileishmanial Activity of a Series of N2,N4-Disubstituted Quinazoline-2,4-diamines

“…18 Bhattacharjee et al ( B ), Ram et al ( C ), and Shakya and Gupta et al ( D and E ) have also tested quinazolines as antileishmanials. 19−22 This class of compounds has been reported as being dihydrofolate reductase (DHFR) inhibitors, although another mechanism of action may be involved with Leishmania . 18,23 Recently, we tested a small library of structurally diverse compounds, originally designed as potential anticancer probes, for antileishmanial activity in a L. mexicana axenic amastigote assay.…”

Discovery of new coumarin substituted quinazolines as potential bioactive agents

“…The initial analog 2,4-dichloroquinazoline (3) was synthesized from 2-nitrobenzoic acid according to the reported literature [13][14][15][16][17][18]. The structure of compound 3 was confirmed by 1 H NMR and 13 C NMR (SI Fig S1-S2) spectrometric analysis.…”

“…1H, -NH),8.34 (d, J = 1.7 Hz, 1H), 7.67-7.29 (m, 8H, Ar-H), 7.04-6.73 (m, 4H, Ar-H),6.03 (s, 1H, coumarin) 13. C NMR (100 MHz, DMSO-d 6 ): d 165.2 (1C, Cquinazoline-O-C), 161.8 (1C, Cquinazoline-NH-C), 160.1 (1C, Cbenzothiazole-NH-C), 159.7 (1C, Ccoumarin-O-C), 153.2 (1C, C=O), 152.Fluorobenzo[d]thiazol-2-yl)amino)quinazolin-4-yl)oxy)-2H-chromen-2-one (5d) White solid, Yield: 73 %, M.P.…”

Piperazine scaffold: A remarkable tool in generation of diverse pharmacological agents

“…% cell survival for these compounds was found to be in the range of 41.11-58.61 [136]. Kumar et al evaluated antiproliferative activity of numerous piperazine derivatives, concluding compound 66 as the most active compound of the series with IC 50 values of 4 and 8.2 µg/mL against KB and C-33A respectively [137]. Patel et al developed a series of piperazine derivatives and evaluated their in vitro anticancer potential against DU-145.…”