Abstract Porous functional metal organic frameworks (MOFs) have showcased their potential in biomedical applications, specifically in drug delivery systems (DDSs), due to high surface area, tailorable pore size, tunable functionality, etc. In this work, the efficient nano drug carrier behavior of a Zn‐MOF is reported for two highly utilized drugs, 5‐fluorouracil and calcein. It exhibits a high drug loading capacity and a slow, sustained release profile as monitored by the spectroscopic and microscopic techniques. Utilizing these two drugs, its good anticancer activity against the human breast cancer MCF‐7 cell is established.