Articles Accepted

DESIGN, SYNTHESIS AND EVALUATION OF 6-SUBSTITUTED-4-HYDROXY-1-(2-SUBSTITUEDACETYL)-3-NITROQUINOLIN-2(1H)-ONE FOR ANTICANCER ACTIVITY.
by Dr. MAMLEDESAI SHIVALINGRAO NAGABHUSHAN, 27 Jun 2019

The present work deals with the synthesis of a series of 6-substituted-4-hydroxy-1-(2- substitued alicyclicaminoacetyl)-3-nitroquinolin-2(1H)-one {IVa-d (1-3)} derivatives and evaluation of their in vitro anticancer activity. Docking study was carried out using EGFR-tyrosine kinase binding site (PDB ID: 1m17) revealed encouraging results. The sequence of reactions consists of the initial synthesis of 6-substituted 4-hydroxyquinolin-2(1H)-ones (Ia-d) which were further subjected to nitration reaction to give 6- substituted-4-hydroxy-3-nitroquinolin-2(1H)-one (IIa-d). Condensation of compounds (IIa-d) with chloroacetyl chloride resulted in 6- substituted-1-(2-chloroacetyl)-4-hydroxy-3-nitroquinolin-2(1H)-one (IIIa-d) which was subjected to substitution reaction using various secondary amines yielded the title compounds {IVa-d (1-3)}. All the synthesized compounds were characterized by IR, NMR and Mass spectral data. All the derivatives were tested for their in vitro anticancer activity using KB (Oral cancer) cell lines. Among all the synthesized compounds, compound (IVc-2) was found to be the most cytotoxic as compared to the other synthesized derivatives, with IC50 values of 0.2406µM/mL against KB cell line.

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October 2019
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