Synthesis and Anti-Melanoma Activity of Acryloyl Pyridinone Analogues.

ABSTRACT: A major challenge for clinical management of melanoma is the prevention and treatment of metastatic disease. Drug discovery efforts over the last 10 years have resulted in several drugs that improve the prognosis of metastatic melanoma; however, most patients develop early resistance to these treatments. We designed and synthesized, through a concise synthetic strategy, a series of hybrid olefin-pyridinone compounds that consist of structural motifs from tamoxifen and ilicicolin H. These compounds were tested against a human melanoma cell line and patient-derived melanoma cells that had metastasized to the brain. Three compounds 7 b, 7 c, and 7 g demonstrated promising activity (IC50=0.4-4.3 μM). Cell cycle analysis demonstrated that 7 b and 7 c induce cell cycle arrest predominantly in th

SUBMITTER: Urbaniak A 

PROVIDER: S-EPMC10984326 | biostudies-literature | 2023 Dec

REPOSITORIES: biostudies-literature