Synthesis of Novel (S)-3-(1-Aminoethyl)-8-pyrimidinyl-2-phenylisoquinolin-1(2 H)-ones by Suzuki-Miyaura Coupling and Their Cell Toxicity Activities

A series of (S)-3-(1-aminoethyl)-8-pyrimidinyl-2-phenylisoquinoline-1(2H)-ones 3a-3k was synthesized in 40-98% yield through Suzuki-Miyaura coupling using Pd(PPh₃)₂Cl₂, Sphos, and K₂CO₃ in THF/H₂O mixed solvent. All newly synthesized compounds were evaluated for cell viability (IC₅₀) against MDA-MB-231, HeLa, and HepG2 cells. The antitumor activities of 3a-3k were improved when various pyrimidine motifs were introduced at position C-8 of the isoquinolinone ring.