Development of novel synthetic strategies for the synthesis of bioactive meroterpenoids

Informazioni relative al progetto

NEOTERP

ID dell’accordo di sovvenzione: 792320

DOI

10.3030/792320

Progetto chiuso

Data della firma CE 22 Marzo 2018

Data di avvio 1 Settembre 2018

Data di completamento 31 Agosto 2020

Finanziato da

• EXCELLENT SCIENCE - Marie Skłodowska-Curie Actions

Costo totale

€ 183 454,80

Contributo UE

€ 183 454,80

Coordinato da

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)

Periodo di rendicontazione: 2018-09-01 al 2020-08-31

Sintesi del contesto e degli obiettivi generali del progetto

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.

Lavoro eseguito dall’inizio del progetto fino alla fine del periodo coperto dalla relazione e principali risultati finora ottenuti

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.

Progressi oltre lo stato dell’arte e potenziale impatto previsto (incluso l’impatto socioeconomico e le implicazioni sociali più ampie del progetto fino ad ora)

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