Hétérocycles à fonction quinone. <b>7</b>. Benzo[<i>f</i>]quinazolinediones‐7,10 à action antitumorale potentielle

Parrot‐Lopez, Hélène; Delacotte, Jean-Michel; Renault, Jean; Cros, S.

doi:10.1002/jhet.5570230415

Cited by 6 publications

(1 citation statement)

References 19 publications

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“…Commercially available trimethoxybenzene was treated with n -butyllithium to generate the requisite orthoanion, which was reacted with various electrophiles to furnish the corresponding alcohols and aldehyde ( 4 , 5 , and 2 ). Alcohols 3 and 6 were generated from aldehyde 2 by reduction and homologation followed by reduction, respectively. , The resulting aromatic rings were nitrated under standard conditions of acetic acid and 70% nitric acid to provide compounds 7 − 10 …”

Section: Resultsmentioning

confidence: 99%

Design, Synthesis, and StructureActivity Relationships for Chimeric Inhibitors of Hsp90

et al. 2006

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Inhibition of the 90 kDa heat shock protein (Hsp90) family of molecular chaperones represents a promising new chemotherapeutic approach toward the treatment of several cancers. Previous studies have demonstrated that the natural products, radicicol and geldanamycin, are potent inhibitors of the Hsp90 N-terminal ATP binding site. The cocrystal structures of these molecules bound to Hsp90 have been determined, and through molecular modeling and superimposition of these ligands, hybrids of radicicol and geldanamycin have been designed. A series of macrocylic chimeras of radicicol and geldanamycin and the corresponding seco-agents have been prepared and evaluated for both antiproliferative activity and their ability to induce Hsp90-dependent client protein degradation.

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Section: Resultsmentioning

confidence: 99%