¹⁷⁷Lu is presently being considered as one of the most promising radionuclide for targeted therapy owing to its suitable decay characteristics. ¹⁷⁷Lu in high radionuclidic purity (99.99%) and moderate specific activity (100–110 TBq/g) was produced using enriched (60.6% ¹⁷⁶Lu) Lu₂O₃ target. The macrocycle 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) is known to form stable complexes with lanthanides. Herein, we describe a novel attempt to introduce ¹⁷⁷Lu in the estradiol moiety through a steroidal–BFCA (Bifunctional Chelating Agent) conjugate. The preparation of a steroid conjugate via coupling of 6 a - amino-17 b -estradiol with a C-functionalized DOTA derivative viz. Ρ-NCS-benzyl-DOTA as a BFCA and thereafter the radiolabel- ling of the conjugate with ¹⁷⁷Lu is reported. Biological activity of the resultant estradiol–DOTA conjugate after radiolabelling was studied by carrying out preliminary in vitro cell uptake studies with MCF-7, human breast carcinoma cell line expressing estrogen receptors as well as binding studies with anti-estradiol antibodies.