Concept

Tricyclic

Related publications (9)

Elucidating and modulating regulatory pathways so as to reprogram the immunosuppressive tumor microenvironment for therapeutic benefit

Glioblastoma (GBM) is the most frequent and highly malignant form of brain cancer. New therapeutic regimens are urgently needed as GBM patients present with a minimal response to currently-approved therapies. The goal of this project is to identify new the ...

EPFL2023

Cancer cell autophagy, reprogrammed macrophages, and remodeled vasculature in glioblastoma triggers tumor immunity

Douglas Hanahan, Krisztian Homicsko, Mélanie Louise Tichet, Agnieszka Alicja Chryplewicz, Ksenya Shchors, Julie Laetitia Scotton

Glioblastoma (GBM) is poorly responsive to therapy and invariably lethal. One conceivable strategy to circumvent this intractability is to co-target distinctive mechanistic components of the disease, aiming to concomitantly disrupt multiple capabilities re ...

2022

Unified divergent strategy towards the total synthesis of the three sub-classes of hasubanan alkaloids

Qian Wang, Jieping Zhu, Guang Li

Elegant asymmetric synthesis of hasubanan alkaloids have been developed over the past decades. However, a divergent approach leading to all three sub-classes of this family of natural products remains unknown. We report herein the realization of such an en ...

2021

Combinatorial targeting of angiogenesis with inducers of autophagy in the treatment of glioblastoma multiforme

Julie Laetitia Scotton

Malignant gliomas represent 80% of tumors developing in the central nervous system, with 50% being glioblastomas (GBM), the most aggressive form of the disease. The benefit from current therapies is very limited, the overall 5-year survival rate of patient ...

EPFL2018

The HDAC inhibitor SAHA improves depressive-like behavior of CRTC1-deficient mice: Possible relevance for treatment-resistant depression

Pierre Magistretti, Jean-René Cardinaux

Major depression is a highly complex disabling psychiatric disorder affecting millions of people worldwide. Despite the availability of several classes of antidepressants, a substantial percentage of patients are unresponsive to these medications. A better ...

Elsevier2016

Involvement of the agmatinergic system in the depressive-like phenotype of the Crtc1 knockout mouse model of depression

Pierre Magistretti, Jean-René Cardinaux

Recent studies implicate the arginine-decarboxylation product agmatine in mood regulation. Agmatine has antidepressant properties in rodent models of depression, and agmatinase (Agmat), the agmatine-degrading enzyme, is upregulated in the brains of mood di ...

Nature Publishing Group2016

Dual Targeting of the Autophagic Regulatory Circuitry in Gliomas with Repurposed Drugs Elicits Cell-Lethal Autophagy and Therapeutic Benefit

Douglas Hanahan, Ksenya Shchors, Aristea Massaras

The associations of tricyclic antidepressants (TCAs) with reduced incidence of gliomas and elevated autophagy in glioma cells motivated investigation in mouse models of gliomagenesis. First, we established that imipramine, a TCA, increased autophagy and co ...

Elsevier2015

Synthetic Study towards Strictamine: The Oxidative Coupling Approach

Qian Wang, Jieping Zhu, Weiwu Ren, Nicholas David Charles Tappin

A synthetic approach featuring a key intramolecular oxidative coupling of a dianion for the formation of the C7–C16 bond was exploited aiming at the synthesis of strictamine. Treatment of substituted tetrahydrocarboline with LHMDS at –78 °C followed by iod ...

Georg Thieme Verlag Kg2013

Three-component synthesis of polysubstituted 6-azaindolines and its tricyclic derivatives

Jieping Zhu

By simply heating a toluene soln. of isocyanoacetamide, amine, and aldehyde, a clean three-component reaction occurred to provide the 6-azaindolines and pyrrolidinone-fused 6-azaindolines. E.g., heating a mixt. of morpholine, heptanal, and isocyanoacetamid ...

2005

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