Research Information System
Bioorganic Chemistry, vol.174, 2026 (SCI-Expanded, Scopus)
As a key mediator of tumor angiogenesis, VEGFR-2 has emerged as a promising therapeutic target for combating cancer. In the present study, a series of 6-substituted-3-(4-(4-(substitutedphenyl/benzyl)piperazin-1-yl)benzylidene) indolin-2-one derivatives ( 2–24 ) were synthesized in good yields and structurally confirmed by IR, NMR, and HRMS analyses. Several compounds exhibited strong VEGFR-2 inhibition, with activities comparable to or exceeding that of sorafenib, but lower than sunitinib. Cytotoxicity assays against MCF-7 breast cancer cells revealed five derivatives ( 4 , 7 , 9 , 10 , and 12 ) more active than doxorubicin along with five additional compounds showing comparable potency. In contrast, the compounds displayed moderate cytotoxic activity against the MDA-MB-231 cell line and none showed significant toxicity toward MCF-10A normal breast epithelial cells. Mechanistic studies of compound 10 demonstrated G0/G1 phase arrest , apoptosis induction, and increased ROS generation , suggesting its potential as a selective and effective lead for breast cancer therapy.