Synthesis and antitumor evaluation of hybrids of 5,8-dioxo-5,8-dihydroisoquinoline-4-carboxylates and carbohydrates.
FUTURE MEDICINAL CHEMISTRY(2018)
摘要
Aim: Cancer has emerged as a growing public health problem in many parts of the world. Methodology: We describe the synthesis of a series of carbohydrate-based isoquinoline-5,8-diones through the 1,4-addition reaction between 5,8-dioxo-5,8-dihydroisoquinoline and aminocarbohydrates. Halogenated quinones were also synthesized. Their inhibitory effects on the proliferation of human cancer cell lines were studied. Results & conclusion: The most promising compound, derived from isoquinoline-5,8-dione, containing ribofuranosidyl ring, was selectively active in vitro against H1299 cancer cells, with 1.7-fold higher activity than that of vinorelbine tartrate. This result suggests that the glycoconjugate in question may constitute a valuable lead compound to design and synthesize a more active and less toxic derivative with respect to the development of a new antitumor substance.
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关键词
aminocarbohydrate,antitumoral activity,halogenated compounds,in vitro assay,isoquinoline-5,8-dione,synthesis
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