Design, Synthesis and Biological Evaluation of Novel Phenylsulfonylurea Derivatives as PI3K/mTOR Dual Inhibitors.

ABSTRACT: Five series of novel phenylsulfonylurea derivatives, 19a⁻d, 20a⁻d, 21a⁻d, 22a⁻d and 23a⁻d, bearing 4-phenylaminoquinoline scaffold were designed, synthesized and their IC₅₀ values against four cancer cell lines (HepG-2, A549, PC-3 and MCF-7) were evaluated. Most compounds showed moderate cytotoxicity activity against the cancer cell lines. Structure⁻activity relationships (SARs) and pharmacological results indicated that introduction of 4-aminoquinoline scaffold and phenylsulfonylurea scaffold were beneficial for anti-tumor activity. Moreover, para-methoxyl substitution of 4-anilino moiety and para-halogen substitution of phenylsulfonylurea have different impacts on different series of compounds. Furthermore,

SUBMITTER: Zhao B 

PROVIDER: S-EPMC6099940 | biostudies-literature | 2018 Jun

REPOSITORIES: biostudies-literature