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(2 H )-ones 3a - 3k was synthesized in 40-98% yield through Suzuki-Miyaura coupling using Pd(PPh 3 ) 2 Cl 2 , Sphos, and K 2 CO 3 in THF/H 2 O mixed solvent. All newly synthesized compounds were evaluated for cell viability (IC 50 ) 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.