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Keeping in view the emerging need for potent and safer anti‐breast cancer agents as well as the pharmacological attributes of isatin, quinolone, and morpholine derivatives, novel hydrazine‐linked morpholinated isatin–quinoline hybrids were designed, synthesized, and evaluated as anti‐breast cancer agents. The synthesized hybrid compounds were preliminarily screened against two breast cancer cell lines (MCF‐7 and MDA‐MB‐231). Almost all synthetics showed potent inhibitory potential against hormone‐positive MCF‐7 cells while being inactive against hormone‐negative MDA‐MB‐231 cells. Potent compounds were further evaluated against the L929 (noncancerous skin fibroblast) cell line and found to be highly selective for MCF‐7 cells over L929 cells. Cell cycle analysis confirmed that the most potent compound AS‐4 (MCF‐7: GI50 = 4.36 µM) causes mitotic arrest at the G2/M phase. Due to higher selectivity toward estrogen receptor alpha (ERα)‐dependent MCF‐7 cells, various binding interactions of AS‐4 with ERα are also streamlined, suggesting the capability of AS‐4 to completely block ERα. Overall, the study suggests that AS‐4 can act as a potential lead for further development of potent and safer anti‐breast cancer agents.

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