Synthesis, Antitubulin, and Antiproliferative SAR of C3/C1??Substituted Tetrahydroisoquinolines

…, R Bai, E Hamel, E Ferrandis, PG Kasprzyk…

Index: Dohle, Wolfgang; Leese, Mathew P.; Jourdan, Fabrice L.; Major, Meriel R.; Bai, Ruoli; Hamel, Ernest; Ferrandis, Eric; Kasprzyk, Philip G.; Fiore, Ann; Newman, Simon P.; Purohit, Atul; Potter, Barry V. L. ChemMedChem, 2014 , vol. 9, # 2 p. 350 - 370

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Citation Number: 5

Abstract

Abstract The syntheses and antiproliferative activities of novel substituted tetrahydroisoquinoline derivatives and their sulfamates are discussed. Biasing of conformational populations through substitution on the tetrahydroisoquinoline core at C1 and C3 has a profound effect on the antiproliferative activity against various cancer cell lines. The C3 methyl-substituted sulfamate (±)-7-methoxy-2-(3-methoxybenzyl)-3-methyl-6 ...