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

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.

SUBMITTER: Santos ARN 

PROVIDER: S-EPMC6786241 | biostudies-literature | 2019 Aug

REPOSITORIES: biostudies-literature

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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 ARN   Sheldrake Helen M HM   Ibrahim Ali I M AIM   Danta Chhanda Charan CC   Bonanni Davide D   Daga Martina M   Oliaro-Bosso Simonetta S   Boschi Donatella D   Lolli Marco L ML   Pors Klaus K  

MedChemComm 20190627 8

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. ...[more]

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