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Exploration of [2 + 2 + 2] cyclotrimerisation methodology to prepare tetrahydroisoquinoline-based compounds with potential aldo-keto reductase 1C3 target affinitySantos, 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 04 September 2019 (has links)
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).
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