Marine Pyrrolocarbazoles and Analogues: Synthesis and Kinase Inhibition

Granulatimide and isogranulatimide are alkaloids obtained from marine sources which have been shown to inhibit cell-cycle G2-checkpoint, targeting more particularly checkpoint 1 kinase (Chk1). At a structural level, they possess a characteristic pyrrolocarbazole framework also shared by the well-known rebeccamycin and staurosporine microbial metabolites which have been described to inhibit topoisomerase I and diverse kinases, respectively. This review reports precisely on the synthesis and kinase inhibitory activities of pyrrolocarbazole-based analogues of granulatimide

Etude d'aza-analogues des alcaloïdes marins de type pyrroloquinoline, wakayine et tsitsikammamines à activité antitumoral potentielle (approche vers la synthèse totale des produits naturels)

TOULOUSE3-BU Sciences (315552104) / SudocSudocFranceF

Synthesis of analogues of the marine pyrroloiminoquinone alkaloid wakayin as potential IDO1 inhibitors

Two strategies have been investigated for the synthesis of the marine alkaloid wakayin resulting in the generation of different intermediates of potential value as inhibitors of indoleamine-2,3-dioxygenase (IDO1), a target enzyme involved in the capacity of tumors to escape the immune process. The first one, based on the condensation of a -hydroxyamine on an indoledione for the formation of the bispyrroloiminoquinone framework, has led to wakayin analogues in which one of the pyrrole ring was not completely aromatic. The second, involving the condensation of methyltryptamine on an indoledione and subsequent oxidative cyclisation of the resulting adduct, allowed to define an original method for constructing the bispyrroloquinoline motif. Different analogues comprising a methyl group on the nitrogen of the pyrrole cycle not constituting the pyrroloiminoquinone unit have been obtained

Synthèse de nouveaux composés N-polyhétéroaromatiques fusionnés basés sur les motifs granulatimide et triazolophthalazine pour leurs propriétés anticancéreuses ou antituberculeuses

TOULOUSE3-BU Sciences (315552104) / SudocSudocFranceF

Synthesis of substituted amido-isogranulatimide analogues as potential checkpoint1 kinase inhibitors

International audienc

Design of granulatimide and isogranulatimide analogues as potential Chk1 inhibitors: Study of amino-platforms for their synthesis

International audienc

New reaction of formation of the fused tricyclic bispyrroloquinone ring system

International audienc

Ascididemin derivatives and their therapeutic applications.

info:eu-repo/semantics/publishe

Phenanthroline-7-one derivatives and their therapeutic uses.

info:eu-repo/semantics/publishe