2009-84-9Relevant articles and documents
Dihydrotestosterone derivatives: Relative binding affinity versus affinity purification
Stobaugh, Mark E.,Blickenstaff, Robert T.
, p. 581 - 585 (1991)
Mono esters of a homologous series of diacids of dihydrotestosterone were synthesized and converted to the corresponding n-butyl amides. The relative binding affinities of these amides to androgen receptor were compared with the degree of purification of rat prostate androgen receptor by affinity columns prepared by linking the steroidal acid to ammo Sepharose. There was good correlation between binding of the amide model to androgen receptor and the extent of purification by the affinity resin.
Method for preparing 8 -methyldialdehyde
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Paragraph 0044-0047; 0054-0057; 0064-0067, (2021/11/03)
To the preparation method of 8 - chloro 6 - hexanol, the hydroxyl is firstly protected with the dihydropyran under the catalysis of p-toluenesulfonic acid, and -1 -chloro 6 -hexyl tetrahydropyranyl is obtained. 6 -chloro -hexyl tetrahydropyranyl ether is reacted with magnesium chips to form a formative reagent and reacted with 1 - bromo -2 - methyl - butane under the catalysis of cuprous bromide to obtain the intermediate 8 - methyl -tetrahydropyran ether. The intermediates do not need to be purified, and the hydroxyl group is removed directly under acidic conditions to obtain 8 - methyl -1 - sunflower. Finally, 2, 2, 6 and 6 - tetramethylpiperidine are oxidized to obtain the product 8 - methyldialdehyde. The synthesis process uses common reagents, is low in cost, mild in reaction conditions and high in yield, is suitable for large-scale industrial production, and has a good application prospect in the field of food additives.
ANTI-CANCER NUCLEAR HORMONE RECEPTOR-TARGETING COMPOUNDS
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Page/Page column 123-124; 142-143, (2021/05/21)
The disclosure relates to anti-cancer compounds which are anti-cancer PARP inhibitors of formula Al, A2, A3 or A4 conjugated by a linker to a steroid, whereby the steroid targets the conjugate to the nucleus, as well as to methods for their preparation and use. (I)
