929193-49-7Relevant articles and documents
2'-carbonyl-3-bromo-spiro[benzofuran-2,4'-oxazolidine] compounds and preparation method thereof
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Paragraph 0157; 0159-0161, (2017/08/02)
The invention discloses 2'-carbonyl-3-bromo-spiro[benzofuran-2, 4'-oxazolidine] compounds and a preparation method thereof. The 2'-carbonyl-3-bromo-spiro[benzofuran-2,4'-oxazolidine] compounds are photoactive compounds shown in the structural formula II. The 2'-carbonyl-3-bromo-spiro[benzofuran-2,4'-oxazolidine] compounds are photoactive spiro compounds, photoactive chiral spiro compounds with multiple functional groups substituted, such as photoactive chiral spiro compounds with azido groups, hydroxyl groups, allyl groups and anisole groups substituted, can be obtained through substitution reactions of bromine atoms at site 3 under different reaction conditions. Therefore, different kinds of other photoactive chiral spiro compounds are prepared by using the substitution reactions of bromine atoms, the range of the compounds is enlarged, and the potential application value is great.
N-(4-(4-(2,3-dichloro- or 2-methoxyphenyl)piperazin-1-yl)butyl) heterobiarylcarboxamides with functionalized linking chains as high affinity and enantioselective D3 receptor antagonists
Newman, Amy Hauck,Grundt, Peter,Cyriac, George,Deschamps, Jeffrey R.,Taylor, Michelle,Kumar, Rakesh,Ho, David,Luedtke, Robert R.
experimental part, p. 2559 - 2570 (2010/03/01)
In the present report, the D3 receptor pharmacophore is modified in the 2,3-diCl- and 2-OCH3-phenyl-piperazine class of compounds with the goal to improve D3 receptor affinity and selectivity. This extension of structure-activity relationships
Evaluation of radiolabeled (Hetero)aromatic analogues of N-(2-diethylaminoethyl)-4-iodobenzamide for imaging and targeted radionuclide therapy of melanoma
Chezal, Jean-Michel,Papon, Janine,Labarre, Pierre,Lartigue, Claire,Galmier, Marie-Josephe,Decombat, Caroline,Chavignon, Olivier,Maublant, Jean,Teulade, Jean-Claude,Madelmont, Jean-Claude,Moins, Nicole
experimental part, p. 3133 - 3144 (2009/04/07)
Targeted radionuclide therapy using radioiodinated compounds with a specific affinity for melanoma tissue is a promising treatment for disseminated melanoma, but the candidate with the ideal kinetic profile remains to be discovered. Targeted radionuclide therapy concentrates the effects on tumor cells, thereby increasing the efficacy and decreasing the morbidity of radiotherapy. In this context, analogues of N-(2-diethylaminoethyl)-4- iodobenzamide (BZA) are of interest. Various (hetero)aromatic analogues 5 of BZA were synthesized and radioiodinated with 125I, and their biodistribution in melanoma-bearing mice was studied after i.v. administration. Most [125I]5-labeled compounds appeared to bind specifically and with moderate-to-high affinity to melanoma tumor. Two compounds, 5h and 5k, stood out with high specific and long-lasting uptake in the tumor, with a 7- and 16-fold higher value than BZA at 72 h, respectively, and kinetic profiles that makes them promising agents for internal targeted radionuclide therapy of melanoma.
