TY - JOUR AU - Desai, S. N. Mamle AU - Priolkar, Rudrax N. S. AU - Karmali, Harshank A. Naik AU - Ambe, Prabhav D. AU - Biradar, B. S. PY - 2017/10/02 Y2 - 2024/03/29 TI - SYNTHESIS, CHARACTERIZATION AND EVALUATION OF 4-HYDROXY-1-PHENYL/METHYL-3-(3-SUBSTITUTED-1-(SUBSTITUTEDIMINO) PROPYL) QUINOLINE-2(1H)-ONE DERIVATIVES AND 4-HYDROXY-1-PHENYL/METHYL-3-(1-(SUBSTITUEDIMINO) ETHYL) QUINOLINE-2(1H)-ONE DERIVATIVES AS POSSIBLE ANTICANCER AGENTS JF - International Journal of Pharmacy and Pharmaceutical Sciences JA - Int J Pharm Pharm Sci VL - 9 IS - 10 SE - Original Article(s) DO - 10.22159/ijpps.2017v9i10.20184 UR - https://journals.innovareacademics.in/index.php/ijpps/article/view/20184 SP - 240-244 AB - <p><strong>Objective: </strong>Synthesis, characterization and evaluation of quinolin-2-one derivatives as possible anticancer agents.</p><p><strong>Methods: </strong>A series of novel 4-hydroxy-1-phenyl/methyl-3-(3-substituted-1-(substitutedimino)propyl)quinolin-2(1<em>H</em>)-one derivatives IIa(1-5)/IIb(1-5) and 4-hydroxy-1-phenyl/methyl-3-(1-(substituedimino)ethyl)quinolin-2(1<em>H</em>)-one derivatives IIIa(1-3)/IIIb(1-3) were synthesised by nucleophilic addition of substituted anilines on 3-acetyl-4-hydroxy-1-phenyl/methylquinolin-2(1<em>H</em>)-one (a/b) and 4-hydroxy-3-(3-substitutedpropanoyl)-1-phenyl/methyl quinolin-2(1<em>H</em>)-one (Ia/Ib); respectively. The synthesised derivatives were characterised by spectral analysis and were tested for their <em>in vitro</em> anticancer activity against K562 and Hep 3b cell lines by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay method.</p><p><strong>Results: </strong>The compounds were tested for their <em>in vitro</em> anticancer activity against K562 and Hep 3b cell lines at 10, 20, 25, 30 and 50 µg/ml concentration using MTT assay method. The compound 4-hydroxy-3-(3-morpholino-1-(phenylimino)propyl)-1-phenylquinolin-2(1<em>H</em>)-one (IIa-1) showed anticancer activity with IC<sub>50 </sub>value 20 µg as compared to the control against K562 cell lines. The compound 4-hydroxy-1-phenyl-3-(1-(phenylimino) ethyl) quinolin-2(1<em>H</em>)-one (IIIa-1) showed anticancer activity with IC<sub>50</sub> value less than 10 µg.</p><p><strong>Conclusion: </strong>The proposed method for the synthesis of novel derivatives is convenient and gives a good yield. Some of the synthesised compounds showed promising anticancer activity against K562 and Hep 3b cell lines. Compound IIa-1 (R=-C<sub>6</sub>H<sub>5</sub>; R<sub>1</sub>= morpholine; R<sub>2</sub>= C<sub>6</sub>H<sub>5</sub>-NH-) exhibited most potent activity against K562 cell lines. Compound IIIa-1 (R=-C<sub>6</sub>H<sub>5</sub>; R<sub>3</sub>= C<sub>6</sub>H<sub>5</sub>-NH-) has been proved to be the most cytotoxic compound among the other derivatives against Hep 3b cell lines.</p> ER -