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

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...

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Veröffentlicht in:	Molecules (Basel, Switzerland) Switzerland), 2020-12, Vol.25 (24), p.5847
Hauptverfasser:	Gujarathi, Satheesh, Zafar, Maroof Khan, Liu, Xingui, Eoff, Robert L, Zheng, Guangrong
Format:	Artikel
Sprache:	eng
Schlagworte:	Analogs Benzopyrans - chemical synthesis Biological Products - chemistry Cancer Chemistry Techniques, Synthetic Chromatography Deoxyribonucleic acid DNA DNA polymerase DNA Polymerase beta - antagonists & inhibitors DNA polymerase β DNA-directed DNA polymerase Drug Design Enzyme Inhibitors - chemical synthesis garcinoic acid Humans Inhibitors Inhibitory Concentration 50 Natural products Phenol - chemistry semi-synthesis Semisynthesis Solvents Structure-Activity Relationship Temperature Vitamin E - analogs & derivatives Vitamin E - chemistry δ-tocotrienol
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Zusammenfassung:	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.
ISSN:	1420-3049 1420-3049
DOI:	10.3390/molecules25245847