New antiproliferative 3-substituted oxindoles inhibiting EGFR/VEGFR-2 and tubulin polymerization.

ABSTRACT: New 3-substituted oxindole derivatives were designed and synthesized as antiproliferative agents. The antiproliferative activity of compounds 6a-j was evaluated against 60 NCI cell lines. Among these tested compounds, compounds 6f and 6g showed remarkable antiproliferative activity, specifically against leukemia and breast cancer cell lines. Compound 6f was the most promising antiproliferative agent against MCF-7 (human breast cancer) with an IC₅₀ value of 14.77 µM compared to 5-fluorouracil (5FU) (IC₅₀ = 2.02 µM). Notably, compound 6f hampered receptor tyrosine EGFR fundamentally with an IC₅₀ value of 1.38 µM, compared to the reference sunitinib with an IC₅₀ value of 0.08 µM. Moreover, compound 6f afforded anti-tubulin polymerization activity wi

SUBMITTER: Ezelarab HAA 

PROVIDER: S-EPMC11070402 | biostudies-literature | 2024 Apr

REPOSITORIES: biostudies-literature