In the present study, the title compound 2‐hydroxy‐N′‐(4,5,6‐trimethoxy‐2,3‐dihydro‐1H‐inden‐1‐ylidene) benzohydrazide (L) was synthesized and its Cu(II), Co(II), Ni(II) and Zn(II) complexes (1–4) were characterized using ultraviolet–Vis, FT‐IR, nuclear magnetic resonance (1H and 13C), electron spin resonance, powder‐X‐ray diffraction, and mass spectral techniques. The investigation on antioxidant activity indicate that the complex 1 and complex 3 have good scavenging activity against various free radicals (2‐diphenyl‐1‐picrylhydrazyl) with IC50 values ranging from 10.14 to 12.16 μg/mL. The in vitro cytotoxicity of these complexes was evaluated using the 3‐4,5‐dimethylthiazole‐2,5‐diphenyltetraazolium bromide assay. The results demonstrate that complexes 1 and 2 show good anticancer activities against human tumor cell line‐7 (breast cancer cell line) and Hep‐G2 (human liver cancer cell line) cell lines with IC50 values of 6.38 and 6.20 μg/mL and that complex 1 is next to complex 2 with IC50 values of 7.26 and 8.15 μg/mL, respectively. The results of antimicrobial activity also suggest that the complex 1 and complex 2 exhibited greater cell death counts for gram positive and gram negative bacterial and antifungal strains with good inhibition values.