Schiff bases and their metal complexes are emerging as key classes of medicinal compounds, possessing an enormous potential of biological activities like anticancer, anticonvulsant and antioxidant etc. The aim of this review is to examine the anticancer activity of different classes of Schiff bases and their metal complexes.Anticancer activity of the already synthesized as well as the novel Schiff bases and their metal complexes was studied using different assays such as 3- [4,5-dimethyltiazol-2-yl]-2,5-diphenyl-tetrazolium bromide (MTT), PI staining, Sulforhodamine, Allium cepa, Sulfo- Rhodamine-B-stain(SRB), viability and potato disc against various human and animal cancer cell lines.The test results indicated significant differences in anticancer activity between subclasses of Schiff base compounds as well as between the Schiff base ligands and their metal complexes. Quinazolines showed a very high activity against HepG2 and MCF-7 cell lines. Pyrazole-naphthalene derivatives exhibited high activity against numerous carcinoma cells while [Ni(HL1)2(OAc)2] showed the highest. Azosal and its tin(IV) complexes displayed high activity against U-1242 MG and excellent activity against HCT-116 cell lines. 2-thiouracil sulfonamides displayed high activity against MCF7, CaCo-2 carcinoma cells. Vitamin-B6 and its oxovanadium complex showed good activity against MCF-7, 3T3 and cervical cancer HeLa cancer cell lines in the presence of visible light. Indoles displayed high activity against AMJ13. Porphyrines derivatives exhibited good activity while its binuclear(Y and K) complexes displayed high activity against several carcinoma cells. Chitosan complexes of [Pd(II) and Pt(II)] showed a very high anticancer activity against MCF-7 carcinoma cell.Schiff bases possess a high potential to inhibit carcinoma cells which enhanced with complexation, but the mechanism of their antitumor activity is still doubt.