Exploration of [2 + 2 + 2] cyclotrimerisation methodology to prepare tetrahydroisoquinoline-based compounds with potential aldo-keto reductase 1C3 target affinity

Description

Yes / Tetrahydroisoquinoline (THIQ) is a key structural component in many biologically active molecules including natural products and synthetic pharmaceuticals. Here, we report on the use of transition-metal mediated [2 + 2 + 2] cyclotrimerisation of alkynes to generate tricyclic THIQs with potential to selectively inhibit AKR1C3. / Fundação para a Ciência, a Tecnologia (PhD studentship ARNS SFRH/BD/46871/2008), EPSRC (RCUK Academic Fellowship HMS), UniTO grant Ricerca Locale 2015 (grant number LOLM_RILO_17_01) and Fondazione Cassa di Risparmio di Torino (grant BOSD_CRT_17_2).

Links & Downloads

1. Santos ARN, Sheldrake HM, Ibrahim AIM et al (2019) Exploration of [2 + 2 + 2] cyclotrimerisation methodology to prepare tetrahydroisoquinoline-based compounds with potential aldo-keto reductase 1C3 target affinity. MedChemComm. 10(8): 1476-1480.
2. http://hdl.handle.net/10454/17252
3. https://doi.org/10.1039/C9MD00201D

Tags

Tetrahydroisoquinoline

THIQ

Additional Fields

Identifer	oai:union.ndltd.org:BRADFORD/oai:bradscholars.brad.ac.uk:10454/17252
Date	04 September 2019
Creators	Santos, Ana R.N., Sheldrake, Helen M., Ibrahim, Ali I.M., Danta, Chhanda C., Bonanni, D., Daga, M., Oliaro-Bosso, s., Boschi, D., Lolli, M.L., Pors, Klaus
Source Sets	Bradford Scholars
Language	English
Detected Language	English
Type	Article, Accepted manuscript
Rights	(c) 2019 RSC. Full-text reproduced in accordance with the publisher's self-archiving policy., Unspecified