Synthesis, Anti??tubulin and Antiproliferative SAR of Steroidomimetic Dihydroisoquinolinones

…, W Dohle, MP Thomas, E Hamel, E Ferrandis…

Index: Leese, Mathew P.; Jourdan, Fabrice L.; Major, Meriel R.; Dohle, Wolfgang; Thomas, Mark P.; Hamel, Ernest; Ferrandis, Eric; Mahon, Mary F.; Newman, Simon P.; Purohit, Atul; Potter, Barry V. L. ChemMedChem, 2014 , vol. 9, # 4 p. 798 - 812

Full Text: HTML

Citation Number: 4

Abstract

Abstract A SAR translation strategy adopted for the discovery of tetrahydroisoquinolinone (THIQ)-based steroidomimetic microtubule disruptors has been extended to dihydroisoquinolinone (DHIQ)-based compounds. A steroid A, B-ring-mimicking DHIQ core was connected to methoxyaryl D-ring mimics through methylene, carbonyl, and sulfonyl linkers, and the resulting compounds were evaluated against two cancer cell lines. The ...