We developed a cost-effective and eco-friendly click biosynthesis of small molecule quercetin-gold quantum dots (QRT-AuQDs) involving quick conjugation using an ultrasonication method at ambient temperature by utilizing QRT and gold ions in the proportion of 0.1 : 1 (molar ratio). A comparatively very short amount of time (60 seconds) was required as compared to conventional procedures. The present biomimetics research relates to the isolation of bioactive QRT by the circularly spread silica gel layer technique (CSSGLT) and characterization (UV-Vis, FTIR, NMR and DSC analysis). Characterization of the synthesized QRT–AuQDs conjugated complex was carried out by UV-Vis, HR-TEM, DLS, zeta potential and X-ray diffraction. The main objective of the present work was to study the comparative anticancer activity of QRT and QRT-AuQDs on human lung cancer HOP-62 and leukemia K-562 cell lines. The results suggested that QRT-AuQDs showed potential for applications in anticancer treatment and were found to be a more cytotoxic agent in comparison to QRT, causing > 50% inhibition of cancer cells at the concentration < 10^-7 M. Hence, small molecule conjugated QRT-AuQDs can be used as a promising material for biomedical, bioengineering and anti-infectives applications.