Development of novel synthetic strategies for the synthesis of bioactive meroterpenoids

Informacje na temat projektu

NEOTERP

Identyfikator umowy o grant: 792320

DOI

10.3030/792320

Projekt został zamknięty

Data podpisania przez KE 22 Marca 2018

Data rozpoczęcia 1 Września 2018

Data zakończenia 31 Sierpnia 2020

Finansowanie w ramach

• EXCELLENT SCIENCE - Marie Skłodowska-Curie Actions

Koszt całkowity

€ 183 454,80

Wkład UE

€ 183 454,80

Koordynowany przez

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)

Okres sprawozdawczy: 2018-09-01 do 2020-08-31

Podsumowanie kontekstu i ogólnych celów projektu

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.

Prace wykonane od początku projektu do końca okresu sprawozdawczego oraz najważniejsze dotychczasowe rezultaty

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.

Innowacyjność oraz oczekiwany potencjalny wpływ (w tym dotychczasowe znaczenie społeczno-gospodarcze i szersze implikacje społeczne projektu)

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