2. Academic Validation
  3. Synthesis of 5-substituted quinazolinone derivatives and their inhibitory activity in vitro

Synthesis of 5-substituted quinazolinone derivatives and their inhibitory activity in vitro

  • Bioorg Med Chem Lett. 1998 Dec 1;8(23):3287-90. doi: 10.1016/s0960-894x(98)00602-7.
D J Baek 1,  Y K Park,  H I Heo,  M Lee,  Z Yang,  M Choi
Affiliations

Affiliation

  • 1 Drug Discovery Lab I, Choongwae Pharma Co., Suwon, Korea.
PMID: 9873719 DOI: 10.1016/s0960-894x(98)00602-7
Abstract

Quinazolinone derivatives I and their methyl esters were synthesized and evaluated as nonclassical lipophilic inhibitors of Thymidylate Synthase. Compounds Ib and Ic containing OH and CO2H as R substituents, respectively, were most effective, indicating that hydrogen bonding may contribute to the increased inhibitory activity. These compounds further showed high cytotoxic activity against tumor cells in culture.

Figures