The leading cause of death worldwide is reportedly cancer. This deadly, multigenetic condition is characterized by unchecked cell proliferation and differentiation. A family of protein kinases known as tyrosine kinases is essential for cancer cell survival and metastasis. The fibroblast growth factor receptor (FGFR), vascular endothelial growth factor receptor (VEGFR), and epidermal growth factor receptor (EGFR) are members of this family of kinases. As a result of medication resistance and systemic toxicity brought on by current cancer treatments, the development of novel anticancer agents is urgently necessary. One of the main goals of creating new, strong anticancer drugs is to prevent angiogenesis by reducing VEGFR-2 activity. The effectiveness of novel synthesised pyrrolotriazolopyrimidine derivatives 6a,b against sixty human cancer cell lines from nine different cancer types was evaluated. The results were analyzed, and molecular docking was used to simulate the inhibitory activity of compounds 6a and b on VEGFR-2. Spectroscopic examination supported the chemical structure of 6a,b.