Synthesis and Characterization of Nonsteroidal Glucocorticoid Receptor Modulators for Multiple Myeloma

Abstract

Structure-activity relationship studies centered around 3'-substituted (Z)-5-(2'-(thienylmethylidene))1,2-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5H-chromeno[3,4-f]quinolines are described. A series of highly potent and efficacious selective glucocorticoid receptor modulators were identified with in vitro activity comparable to dexamethasone. In vivo evaluation of these compounds utilizing a 28 day mouse tumor xenograft model demonstrated efficacy equal to dexamethasone in the reduction of tumor volume.

Selective Glucocorticoid Receptor modulators

“…Of note, the therapeutic advantages of non-steroidal GR agonists over classic GCs are being explored not only for anti-inflammatory diseases but also for the purpose of treating cancers, including multiple myeloma or prostate cancer [67,68].…”

Synthesis of Novel Fragrant Molecules 6-Methoxy-2,6-dimethyl Heptanol Derivatives

“…However, these elegant synthesis are not so easy to perform. As for bromocyclohexane and bromo-cyclopentane 19,20 , whose Grignard reagents don't react with 4 in the temperature of 0-10 °C, but undergo coupling a GC Content is based on the addition reaction of 4 with the correspondent Grignard reagents. b Purity is the GC content after purification.…”

2‐Iodoxybenzoesäure – ein einfaches Oxidationsmittel mit einer Vielfalt an Anwendungsmöglichkeiten

“…[57] Zudem toleriert die IBX-Oxidation von Alkoholen eine große Bandbreite weiterer Funktionalitäten wie beispielsweise: Allene, [60] Azide, [61] Cyclopropane, [62] Diazoverbindungen, [63] Epoxide, [64,65] Phosphate, [66] Phosphonate, [67] Silane, [68] Germane, [69] Stannane, [70] Trifluorborate, [71] Eisen-und Rheniumkomplexe [72,73] sowie zahlreiche stickstoff-und schwefelhaltige Heterocyclen. [74][75][76][77][78][79][80][81][82][83][84] Auch die Kompatibilität mit den meisten gängigen Schutzgruppen führt zu einer ständig wachsenden Zahl an Anwendungen in der Synthese.…”