ALS-007
Chemical Name: 12-(beta-D-Glucopyranosyl)-3,9-dihydroxy-6,7,12,13-tetrahydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7-dione
项目整合开发状态: Biological Testing
项目研究机构: Advanced Life Sciences (Originator)
合成路线:Condensation of the magnesium iodide salt of 5-(benzyloxy)indole (I) with N-(benzyloxymethyl)-3,4-dibromomaleimide (II) provided the monoindolyl maleimide (III).Coupling of (III) with the benzyl-protected glucose (IV) via Mitsunobu reaction afforded the glycosylated indole (V).A second indolyl group was then introduced in (V) to give the bisindolylmaleimide (VI),which was oxidatively cyclized to the indolocarbazole (VII) using palladium bis(trifluoroacetate).Finally,hydrogenolysis of the benzyl protecting groups of (VII) over Pd/C furnished the title compound.
📌 参考资料/链接:
参考文献标题:Indolocarbazole poisons of human topoisomerase I: Regioisomeric analogues of ED-110
文献作者:Zembower,D.E.; Zhang,H.; Lineswala,J.P.; Kuffel,M.J.; Aytes,S.A.; Ames,M.M.
参考来源:Bioorg Med Chem Lett 1999,9(2),145