Development of novel synthetic strategies for the synthesis of bioactive meroterpenoids

Información del proyecto

NEOTERP

Identificador del acuerdo de subvención: 792320

DOI

10.3030/792320

Proyecto cerrado

Fecha de la firma de la CE 22 Marzo 2018

Fecha de inicio 1 Septiembre 2018

Fecha de finalización 31 Agosto 2020

Financiado con arreglo a

• EXCELLENT SCIENCE - Marie Skłodowska-Curie Actions

Coste total

€ 183 454,80

Aportación de la UE

€ 183 454,80

Coordinado por

IMPERIAL COLLEGE OF SCIENCE TECHNOLOGY AND MEDICINE
United Kingdom

Periodic Reporting for period 1 - NEOTERP (Development of novel synthetic strategies for the synthesis of bioactive meroterpenoids)

Período documentado: 2018-09-01 hasta 2020-08-31

Resumen del contexto y de los objetivos generales del proyecto

The project concerns the development of innovative methodologies for the synthesis of novel bioactive natural products analogues. Thus, the aim of this project is to devise concise synthetic routes for the total synthesis of bioactive meroterpenoids natural products and their analogueues in order to fully explore their potential application for the discovery of new medicines to treat resistant cancers and resistant microbial infections. In particular, polyenes cyclisation via radical-cations intermediates initiated by photoredox catalysis or deriving from substrate that can readily form electrondeficient carbon centres is a highly promising way to induce such a kind of reactivity in substrates not containing strained cyclic “electron-sink” groups.

Trabajo realizado desde el comienzo del proyecto hasta el final del período abarcado por el informe y los principales resultados hasta la fecha

Despite the high-impact CoViD19 disruptions, novel open-chain resorcylate-merotepenoids, have been synthesised. They can be screened in HTS campaigns for their biological activity or used as intermediate in library generation and additional synthetic studies. High resolution mass spectrometric and HPLC evidence about the cyclisation of one of the substrates were gathered.

Avances que van más allá del estado de la técnica e impacto potencial esperado (incluida la repercusión socioeconómica y las implicaciones sociales más amplias del proyecto hasta la fecha)

High resolution mass spectrometric and HPLC evidence about the cyclisation of one of the substrates support the starting intuition of using novel “electron sink” moieties to trigger polycyclisation reactions. Further development can arise in the future, isolating products from this same reaction or applying the concept to different electron-deficient structures.
The novel open-chain meroterpenoids are suitable for further derivatisation and library development campaign.

Summary Picture