Oncological diseases are one of the most common public health problems and second leading cause of death after cardiovascular disease. Natural products or synthetic compounds inspired from natural products continue to be excellent sources for new drug candidates. Isoxazole and oxazole rings containing nitrogen and oxygen atoms are considered as one of prime scaffolds for the drug discovery. Their structural features make it possible for multiple weak non-covalent interactions such as hydrogen bonds, coordination bonds, π-π stacking, hydrophilic interactions and so on. Such in medicinal chemistry isoxazole and oxazole compounds could readily bind with a variety of enzymes and receptors in biological systems and show broad biological activities like antibacterial, antifungal, antiviral, antitubercular, anticancer, anti-inflammatory and so on. Series of heterocyclic compounds containing pyrrolo[3,4-d]isoxazole framework have been studied for their antiproliferative activity against human cervical carcinoma (HeLa), murine fibroblast (3T3) and SV-40 transformed murine fibroblast (3T3-SV40) cell lines. It was found using confocal microscopy that granular actin was distributed diffusely in the cytoplasm in up to 71% of treated cells after their treatment with tested compounds while actin filaments were disappeared. Number of cells with filopodium-like membrane protrusions was significantly reduced after treatment with some of tested compounds (from 92 % in control cells up to 18% after treatment). The obtained results support the antitumor effect of the studied compounds and encourage the extension of the study in order to improve the anticancer activity and reduce the toxicological risks of obtained compounds.