Novel Pyrazoline and Pyrazoline–Thiazole Derivatives Linked to Tetrahydronaphthalene Ring: Synthesis, Anticancer Evaluation, VEGFR ‐2 Inhibition Activity, and Molecular Docking Study

ABSTRACT A new series of pyrazoline and pyrazoline–thiazole derivatives conjugated with tetralin ring 5a, b–19 was created starting with the chalcones 3a , b . The new compounds were tested as potential anticancer agents on three human cancer cell lines (HCT‐116, HepG‐2, and MCF‐7) and one human normal cell line (BJ‐1). The Compounds 5a , b , 7a , 9a , b , 10 , 13a , d , and 16b were identified as strong candidates against the MCF‐7 cell line (IC 50 = 2.0 ± 0.1–5.6 ± 0.2 μM), where all the compounds exhibited significant activity against the HCT‐116 cell line (IC 50 = 2.8 ± 0.1–6.5 ± 0.5 μM). Compounds 5b, 9b , and 10 were chosen to study VEGFR‐2 inhibitors in comparison with sorafenib (IC 50 = 2.9 ± 0.08, 8.6 ± 0.41, 1.1 ± 0.04, and 0.2 ± 0.01 nM, respectively). A molecular docking study was conducted to ascertain the latter compounds' binding interactions with VEGFR‐2 kinase.