Parallel solution phase synthesis of 3,6,7-4(3H)-quinazolinones and evaluation of their antitumor activities against human cancer.

Three diversity points of 4(3H)-quinazolinone are introduced at the 3-, 6-, and 7-positions with an efficient parallel solution-phase synthetic method. A one-pot synthesis was developed that gave the key intermediate in high yield. Five hit compounds exhibit preferable activities against a panel of human tumor cell lines, which pointed out preliminary structure-activity relationships.