Tetrahydroisoquinolinone-Based Steroidomimetic and Chimeric Microtubule Disruptors

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 mi...

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Veröffentlicht in:	ChemMedChem 2014-01, Vol.9 (1), p.85-108
Hauptverfasser:	Leese, Mathew P., Jourdan, Fabrice L., Major, Meriel R., Dohle, Wolfgang, Hamel, Ernest, Ferrandis, Eric, Fiore, Ann, Kasprzyk, Philip G., Potter, Barry V. L.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Antineoplastic Agents - therapeutic use Benzyl Compounds - chemistry Benzyl Compounds - pharmacology Benzyl Compounds - therapeutic use Cell Line, Tumor Cell Proliferation - drug effects colchicine binding Humans Isoquinolines - chemistry Isoquinolines - pharmacology Isoquinolines - therapeutic use Mice Mice, Nude microtubule disruptors Microtubules - chemistry Microtubules - metabolism Multiple Myeloma - drug therapy Multiple Myeloma - metabolism Multiple Myeloma - pathology Stereoisomerism Structure-Activity Relationship tetrahydroisoquinolines Tetrahydroisoquinolines - chemistry Transplantation, Heterologous tubulin assembly Tubulin Modulators - chemistry Tubulin Modulators - pharmacology Tubulin Modulators - therapeutic use
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