Development of trisubstituted thiophene-3-arboxamide selenide derivatives as novel EGFR kinase inhibitors with cytotoxic activity.

ABSTRACT: Overexpression of EGFR is one of the eminent oncogenic drivers detected in the development of several human cancers. The increasing incidences of mutation-based resistance in the tyrosine kinase domain call upon the need for the development of a newer class of small-molecule TK inhibitors. Accordingly, a new series of symmetrical trisubstituted thiophene-3-carboxamide selenide derivatives was developed via the hybridization of complementary pharmacophores. Most of the compounds showed a modest to excellent antiproliferative action at 20 μM concentration. The utmost antiproliferative activity was portrayed by compound 16e on the selected cancer cell lines with IC₅₀ < 9 μM, the lowest being 3.20 ± 0.12 μM in the HCT116 cell line. Further, it also displayed an impressive EGF

SUBMITTER: Makhal PN 

PROVIDER: S-EPMC10718591 | biostudies-literature | 2023 Dec

REPOSITORIES: biostudies-literature