Newly synthesized 6-substituted piperazine/phenyl-9-cyclopentyl containing purine nucleobase analogs act as potent anticancer agents and induce apoptosis via inhibiting Src in hepatocellular carcinoma cells.

ABSTRACT: Newly synthesized 6-substituted piperazine/phenyl-9-cyclopentyl-containing purine nucleobase analogs were tested for their in vitro anticancer activity against human cancer cells. Compounds 15, 17-24, 49, and 56 with IC₅₀ values less than 10 μM were selected for further examination on an enlarged panel of liver cancer cell lines. Experiments revealed that compound 19 utilizes its high cytotoxic potential (IC₅₀ < 5 μM) to induce apoptosis in vitro. Compound 19 displayed a KINOMEscan selectivity score S₃₅ of 0.02 and S₁₀ of 0.01 and demonstrated a significant selectivity against anaplastic lymphoma kinase (ALK) and Bruton's tyrosine kinase (BTK) over other kinases. Compounds 19, 21, 22, 23, and 56 complexed with ALK, BTK

SUBMITTER: Bilget Guven E 

PROVIDER: S-EPMC10718522 | biostudies-literature | 2023 Dec

REPOSITORIES: biostudies-literature