Sideritis niveotomentosa Hub.-Mor. is a local endemic species belonging to the Lamiaceae family. In this study, GC/MS analysis, total antioxidant capacity and anticancer effects of different extracts obtained from S. niveotomentosa were investigated comparatively. Total phenolic contents of extracts were determined by the Folin–Ciocalteu method, total flavonoid contents by aluminum chloride method, and also the free radical scavenging activities of the extracts by DPPH (2,2-diphenyl1-picryl-hydrazyl-hydrate) assay. The cytotoxic effect of the extracts was studied via MTT (3-(4,5Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide) assay on DLD1, HL60 and ARH77 cell lines. Pro-apoptotic gene expression levels were also tested in the most sensitive cell line ARH77 by Real-Time PCR. The expression levels of 4 pro-apoptotic genes, APAF, BAX, CASP3, and HRK were found to be upregulated in ARH77 cells that were treated extracts. Results showed that methanolic extracts contain more phenolic content than acetone extracts, consistent with DPPH results. As a result, Sideritis niveotomentosa extracts, especially methanolic extracts, are rich in phenolic content and have a strong radical scavenging effect. In addition, the extracts showed selective effects on cell lines. This study is pioneering in terms of future studies, and the findings provide hope for future experimentation.