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This research aimed to produce new 1-[(aryl)(3-amino-5-oxopyrazolidin-4-ylidene) methyl]-2-oxo-1,2-dihydroquinoline-3-carboxylic acid derivatives and check their anticancer effect against the breast cancer MCF-7 cell line. The 2-oxo-1,2-dihydroquinoline-3-carboxylic acid (<b>4</b>) compound was obtained by hydrolyzing ethyl 2-oxo-1,2-dihydroquinoline-3-carboxylate (<b>2</b>) with thiourea and anhydrous potassium carbonate ethanol, which was then treated with ethyl 3-substituted 2-cyanoacrylates (<b>6</b>) in the presence of triethylamine in diethyl formamide to give 1-[2-(ethoxy)carbonyl-2-cyano-1-arylvinyl]-2-oxo-1,2-dihydroquinoline-3-carboxylic (<b>7a</b>,<b>d</b>). Cyclization of compound 7 with hydrazine hydrate ethanol inferred the association of 1-[(aryl)(3 amino-5-oxopyrazolidin-4-ylidene)methyl-2-oxo-1,2-dihydroquinol-3-carboxylates (<b>8a</b>,<b>d</b>). Spectroscopic and micro-analytical techniques such as IR, NMR, and elemental analysis were used to validate the structure of the synthesized organic compounds. The anticancer effects of the synthesized compounds <b>7a</b>–<b>d</b> and <b>8a</b>–<b>d</b> were tested by using the MTT assay on the MCF-7 cell line. When compared to the reference compound Dox, the compounds <b>7b</b>,<b>c</b> and <b>8a</b>–<b>c</b> demonstrated strong anticancer activity against the MCF-7 cell line. The anticancer effects of the synthesized compounds <b>7a</b>–<b>d</b> and <b>8a</b>–<b>d</b> were tested against the MCF-7 cell line, using MTT assay. The compounds <b>7b</b>,<b>c</b> and <b>8a</b>–<b>c</b> showed significant anticancer activity compared to the reference compound Dox against the MCF-7 cell line.