Transforming rhinacanthin analogues from potent anticancer agents into potent antimalarial agents

N Kongkathip, N Pradidphol, K Hasitapan…

Index: Kongkathip, Ngampong; Pradidphol, Narathip; Hasitapan, Komkrit; Grigg, Ronald; Kao, Wei-Chun; Hunte, Carola; Fisher, Nicholas; Warman, Ashley J.; Biagini, Giancarlo A.; Kongsaeree, Palangpon; Chuawong, Pitak; Kongkathip, Boonsong Journal of Medicinal Chemistry, 2010 , vol. 53, # 3 p. 1211 - 1221

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Citation Number: 22

Abstract

Twenty-six novel naphthoquinone aliphatic esters were synthesized by esterification of 1, 4- naphthoquinone alcohols with various aliphatic acids. The 1, 4-naphthoquinone alcohols were prepared from 1-hydroxy-2-naphthoic acid in nine steps with excellent yields. Twenty- four of the novel synthetic naphthoquinone esters showed significant antimalarial activity with IC50 values in the range of 0.03− 16.63 μM. The length of the aliphatic chain and the ...