Tetrahydroisoquinolinone??Based Steroidomimetic and Chimeric Microtubule Disruptors

…, E Hamel, E Ferrandis, A Fiore, PG Kasprzyk…

Index: Leese, Mathew P.; Jourdan, Fabrice L.; Major, Meriel R.; Dohle, Wolfgang; Hamel, Ernest; Ferrandis, Eric; Fiore, Ann; Kasprzyk, Philip G.; Potter, Barry V. L. ChemMedChem, 2014 , vol. 9, # 1 p. 85 - 108

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Citation Number: 3

Abstract

Abstract A structure–activity relationship (SAR) translation strategy was used for the discovery of tetrahydroisoquinoline (THIQ)-based steroidomimetic and chimeric microtubule disruptors based upon a steroidal starting point. A steroid A, B-ring-mimicking THIQ core was connected to methoxyaryl D-ring ring mimics through methylene, carbonyl and sulfonyl linkers to afford a number of steroidomimetic hits (eg, 7-methoxy-2-(3-methoxybenzyl)-6- ...