A series of novel 1-thiazolyl-5-coumarin-3-yl-pyrazole derivatives (4a-l) were synthesized via one-pot multicomponent reaction of 5-substituted salicylaldehydes (1a-c), 4-hydroxy-6-methyl-2H-pyran-2-one (2) and 2-hydrazinyl-4-arylthiazoles (3a-d) in acetonitrile using a catalytic amount of piperidine under reflux conditions. This multicomponent approach has advantages such as reduced reaction time and a high product yield percentage when compared with corresponding multistep approaches. All the synthesized compounds were evaluated for their cytotoxic activity against Hep G2 (hepatocellular liver carcinoma) and MCF-7 (breast cancer) cell lines and compared with the standard drug Doxorubicin. Among all the compounds, compounds 4d against Hep G2, 4k against MCF-7 and 4e against both Hep G2 & MCF-7 showed excellent cytotoxic activity.
A novel series of ethyl‐2‐(3‐((2‐(4‐(4‐aryl)thiazol‐2‐yl)hydrazono)methyl)‐4‐hydroxy/isobutoxyphenyl)‐4‐methylthiazole‐5‐carboxylate derivatives (4a‐f and 5a‐f) were synthesized by employing one‐pot multi‐component approach involving ethyl 2‐(3‐formyl‐4‐oxy/isobutoxyphenyl)‐4‐methylthiazole‐5‐carboxylate, thiosemicarbazide and various phenacyl bromides/3‐(2‐bromoacetyl)‐2H‐chromen‐2‐one/2‐(2‐bromoacetyl)‐3H‐benzo[f]chromen‐3‐onein ethanol in the presence of catalytic amount of acetic acid. The structures of all the synthesized compounds were confirmed with spectral analysis, ie, IR, 1H NMR, 13C NMR and mass spectrometry, and all the compounds were screened for their in vitro antimicrobial activity.
Synthesis of Fused 3,4-Dihydropyrimidin-2(1H)-ones and Thiones under Solvent--Free Conditions. -The ionic liquid catalyst is recycled and reused in five consecutive cycles with marginal loss of its activity. -(VELPULA, R.; BANOTHU, J.; GALI, R.; DESHINENI, R.; BAVANTULA*, R.; Chin. Chem. Lett. 26 (2015) 3, 309-312, http://dx.
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