Bassia indica (Wight) A.J. Scott, family Amaranthaceae, is a halophyte herb growing in extreme environments and hence deemed as a potential economic source of bioactive chemicals with functional properties. In our study, 25 compounds were obtained from B. indica. We aimed to assess the inhibitory effect of the methanol extract of B. indica and its isolated compounds on COX-2 and cytotoxicity activity against MCF-7, OVK-18, HepG2, and HCT116 tumor cells. Among the isolates, the triterpene oleanane saponin (23) displayed promising anti-inflammatory activity with an IC 50 = 3.05 ± 0.15 μg/mL. Additionally, N- trans-feruloyl tyramine (11) exhibited significant cytotoxicity to OVK-18 with IC 50 = 1.74 ± 1.56 μg/mL, whereas 6,7-dihydroxy coumarin (7) exhibited potent inhibition against the MCF-7 cell line with IC 50 = 1.47 ± 0.22 μg/mL. Interestingly, compounds 1 and 25 exhibited remarkable cytotoxicity against HepG2 and HCT116 cells with IC 50 < 0.1 μg/mL, while compounds 2, 4, 5, 6, and 9 exerted potent cytotoxicity against HepG2. Finally, B. indica is a potential source of candidate compounds for the development of anti-inflammatory and antitumor therapies.