This research aimed to study the phytochemical and biological properties of eleven clone cultivars of C. variegatum (Mrs. Iceton or Red Iceton, Gold star, Petra, Oak leaf, Norma, Eleanor Roosevelt, Spirale, Majesticum, Zanzibar pictum spot, Andreanum, Red spot) to evaluate their therapeutic potentials, values, and variability. Methanol-soluble portion (MSP) of the total 70% aqueous methanol aerial parts extracts wasprepared using conventional techniques (low temp., low pressure) to prevent the degradation of their active metabolites. Their phytochemical screening and chromatographic analysis revealed the presence of a high content of terpenes, flavonoids, alkaloids, phenolic acids, and saponins. Moreover, the LC-MS technique, using UPLC-qTOF ESI-MS/MS was optimized for the tentative identification of 114 phytoconstituents from the MSP of C. variegatum Zanzibar (Pictum spot) as a representative instance for all eleven cultivars investigated. The identification is mainly based on matching their R_t-values, monoisotopic molecular, specific fragment ion masses, and their relative abundances with the respectable open library database software. The antioxidant activity for MSP of the eleven C. variegatum cultivars revealed a promising antioxidant capacity due to their high polyphenolic content, especially flavonoids and phenolic acids detected by preliminary and LC-MS/MS phytochemical screening. Moreover, a significant effect was noticed for all examined cultivars on the viability of Ehrlich ascites carcinoma cells (EACC), which reflects their antitumor activity. The promising in vitro antioxidant and cytotoxicity findings of the target 11MSP revealed strong broad-spectrum activities that were encouraging to extend special attention to the isolation and biological evaluation of the major constitutive polyphenols as antioxidant and anticancer agents. Current findings draw attention to the fact that C. variegatum Zanzibar can be considered a potent, safe antioxidant and antitumor agent that could be used in many pharmaceutical, food, and folk medicine applications to treat certain diseases.