000			a
999			_c11262 _d11262
003			OSt
005			20200214114505.0
008			200214b xxu||||| |||| 00| 0 eng d
040			_aAIKTC-KRRC _cAIKTC-KRRC
100			_912268 _aBhatt, S. S.
245			_aDESIGN, SYNTHESIS AND EVALUATION OF 6-SUBSTITUTED-4-HYDROXY-1-(2- SUBSTITUTEDACETYL)-3-NITROQUINOLIN-2(1H)-ONEs FOR ANTICANCER ACTIVITY
250			_aVol.56(12), Dec
260			_aMumbai _bIndian Drug Manufacture's Association - IDMA _c2019
300			_a20-27p.
520			_aThe 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) and 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 to yield 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 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.
650		0	_94639 _aPHARMACEUTICS
700			_912270 _aMaleDesai, S. N.
773	0		_tIndian drugs _dMumbai Indian Drug Manufactures Association
856			_uhttp://www.indiandrugsonline.org/issuesarticle-details?id=MTAwMQ== _yClick here
942			_2ddc _cAR