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

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.
Publication Date
2019-01
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(c) 2019 RSC. Full-text reproduced in accordance with the publisher's self-archiving policy.
Peer-Reviewed
Yes
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openAccess
Accepted for publication
2019-06-27
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Abstract
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.
Version
Accepted manuscript
Citation
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.
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