Synthesis and Antitumor Activity of Erlotinib Derivatives Linked With 1,2,3-Triazole.

ABSTRACT: Cervical cancer is one of the most important cause of cancer-related death and presents a major public health problem in many countries. To search for more novel antitumor agents against cervical cancer, 14 erlotinib-linked 1,2,3-triazole compounds were designed, synthesized, and evaluated for their anti-tumor activity. The compounds were confirmed by ¹H NMR, ¹³C NMR, and high-resolution mass spectra (HR MS). Antitumor activity assay results indicated that six of those compounds have remarkable inhibitory activity against human cervical cancer HeLa cells in vitro, among which compound 4m was the most potent with IC₅₀ of 3.79 μM, and compounds 4k, 4i, 4l, 4d, and 4n also demonstrated remarkable antitumor activity with IC₅₀ of 3.79, 4.16, 4.

SUBMITTER: Deng P 

PROVIDER: S-EPMC8802806 | biostudies-literature | 2021

REPOSITORIES: biostudies-literature