Dickens, Michael P. published the artcile5-Deazaflavin derivatives as inhibitors of p53 ubiquitination by HDM2, Application In Synthesis of 93118-03-7, the main research area is deazaflavin derivative preparation p53 ubiquitination inhibitor SAR; Cancer; Deazaflavin; HDM2–p53; Ubiquitin E3 ligase; Ubiquitination inhibitors.
Based on previous reports of certain 5-deazaflavin derivatives being capable of activating the tumor suppressor p53 in cancer cells through inhibition of the p53-specific ubiquitin E3 ligase HDM2, we have conducted an structure-activity relation (SAR) anal. through systematic modification of the 5-deazaflavin template. This anal. shows that HDM2-inhibitory activity depends on a combination of factors. The most active compounds (e.g., I) contain a trifluoromethyl or chloro substituent at the deazaflavin C9 position and this activity depends to a large extent on the presence of at least one addnl. halogen or Me substituent of the Ph group at N10. Our SAR results, in combination with the HDM2 RING domain receptor recognition model we present, form the basis for the design of drug-like and potent activators of p53 for potential cancer therapy.
Bioorganic & Medicinal Chemistry published new progress about Antitumor agents. 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, Application In Synthesis of 93118-03-7.
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