A Facile Semisynthesis and Evaluation of Garcinoic Acid and Its Analogs for the Inhibition of Human DNA Polymerase β

Molecules

RobertL. Eoff¹  MaroofKhan Zafar¹  Xingui Liu²  Guangrong Zheng²  Satheesh Gujarathi² 

[1] Department of Biochemistry and Molecular Biology, College of Medicine, University of Arkansas for Medical Sciences, Little Rock, AR 72205, USA;Department of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, AR 72205, USA;

关键词: garcinoic acid;    δ-tocotrienol;    DNA polymerase β;    structure-activity-relationship;    semi-synthesis;   

DOI  :  10.3390/molecules25245847

来源: DOAJ

【 摘 要 】

Garcinoic acid has been identified as an inhibitor of DNA polymerase β (pol β). However, no structure-activity relationship (SAR) studies of garcinoic acid as a pol β inhibitor have been conducted, in part due to the lack of an efficient synthetic method for this natural product and its analogs. We developed an efficient semi-synthetic method for garcinoic acid and its analogs by starting from natural product δ-tocotrienol. Our preliminary SAR studies provided a valuable insight into future discovery of garcinoic acid-based pol β inhibitors.

【 授权许可】

Unknown