Synthesis of luffariellolide derivatives and evaluation their anticancer activities

Title
Synthesis of luffariellolide derivatives and evaluation their anticancer activities
Author(s)
류민석; 신아영; 이지훈
KIOST Author(s)
Shin, A Young(신아영)Lee, Jihoon(이지훈)
Publication Year
2018-10-18
Abstract
Luffariellolide was isolated from the marine sponge Suberea sp. in a large quantity (> 300 mg). We conducted modification of the γ-hydroxybutenolide core of luffariellolide to synthesize 13 derivatives, using readily available nucleophiles. As a result, some of the pyridazinone analogues were exhibited increased anticancer activities against A375SM (melanonma). Especially, the synthetic derivative, bearing 2-(pyridin-2-yl) pyridazinone, exhibited almost four times higher anticancer activity (IC50 = 6.35 μM) compared to that of luffariellolide (IC50 = 24.4 μM).. As a result, some of the pyridazinone analogues were exhibited increased anticancer activities against A375SM (melanonma). Especially, the synthetic derivative, bearing 2-(pyridin-2-yl) pyridazinone, exhibited almost four times higher anticancer activity (IC50 = 6.35 μM) compared to that of luffariellolide (IC50 = 24.4 μM).
URI
https://sciwatch.kiost.ac.kr/handle/2020.kiost/23029
Bibliographic Citation
대한약학회, pp.327, 2018
Publisher
대한약학회
Type
Conference
Language
English
Publisher
대한약학회
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