1123-61-1Relevant articles and documents
N,N′-Dimethyl-1,4-dithiine-1,2:4,5-tetracarboximide and N,N′-dimethyl-1,4-diselenine-1,2:4,5-tetracarboximide
Brisse, Francois,Atfani, Mohamed,Bergeron, Jean-Yves,Belanger-Gariepy, Francine,Armand, Michel
, p. 190 - 192 (2000)
-
Synthesis and Characterization of the Selective, Reversible PKCβ Inhibitor (9 S)-9-[(Dimethylamino)methyl]-6,7,10,11-tetrahydro-9 H,18 H-5,21:12,17-dimethenodibenzo[ e,k]pyrrolo[3,4- h][1,4,13]oxadiazacyclohexadecine-18,20(19 H)-dione, Ruboxistaurin (LY333531)
Lewin, Anita H.,Brieaddy, Larry,Deschamps, Jeffrey R.,Imler, Gregory H.,Mascarella, S. Wayne,Reddy, P. Anantha,Carroll, F. Ivy
, p. 246 - 251 (2018/09/25)
The demonstrated role of PKCβ in mediating amphetamine-stimulated dopamine efflux, which regulates amphetamine-induced dopamine transporter trafficking and activity, has promoted the research use of the selective, reversible PKCβ inhibitor (9S)-9-[(dimethylamino)methyl]-6,7,10,11-tetrahydro-9H,18H-5,21:12,17-dimethenodibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecine-18,20(19H)-dione, ruboxistaurin. Despite the interest in development of ruboxistaurin as the mesylate monohydrate (Arxxant) for the treatment of diabetic retinopathy, macular edema, and nephoropathy, several crucial details in physicochemical characterization were erroneous or missing. This report describes the synthesis and full characterization of ruboxistaurin free base (as a monohydrate), including X-ray crystallography to confirm the absolute configuration, and of the mesylate salt, isolated as a hydrate containing 1.5 mol of water per mole.
Indolo[2, 3-a]pyrrole[3, 4-c]carbazole-5, 7-dione-6-arylhydrazone compound and its preparation method and use in anti-cancer drug
-
Paragraph 0050; 0051; 0052; 0053; 0054, (2017/08/28)
The invention discloses an indolo[2, 3-a]pyrrole[3, 4-c]carbazole-5, 7-dione-6-arylhydrazone compound and its preparation method and use. The indolo[2, 3-a]pyrrole[3, 4-c]carbazole-5, 7-dione-6-arylhydrazone compound is prepared from an aldehyde compound R-CHO and 6-amino-indolo[2, 3-a]pyrrole[3, 4-c]carbazole-5, 7-dione as raw materials and has a general structural formula shown in the description. The invention also discloses a preparation method of the indolo[2, 3-a]pyrrole[3, 4-c]carbazole-5, 7-dione-6-arylhydrazone compound and a use of the indolo[2, 3-a]pyrrole[3, 4-c]carbazole-5, 7-dione-6-arylhydrazone compound in preparation of anti-cancer drugs. The preparation method has the advantages of easily available raw materials and simple processes. The indolo[2, 3-a]pyrrole[3, 4-c]carbazole-5, 7-dione-6-arylhydrazone compound has good biological activity and has a good application prospect in preparation of anti-cancer drug compounds.
3. 4 - b (3 - indole) - 2, 5 - dione -3 - pyrroline imine compound and its preparation method and application
-
Paragraph 0042; 0043; 0044; 0045; 0046, (2017/07/25)
The invention discloses a 3,4-bi(3-indole)-2,5-dione-3-pyrrolineimine compound, a preparation method of the compound and application of the compound in an anti-cancer drug. The key points of the technical scheme are that the 3,4-bi(3-indole)-2,5-dione-3-pyrrolineimine compound is prepared by taking an aldehyde compound R-CHO and 1-amino-3,4-bi(3-indole)-3-pyrroline-2,5-dione with the structural formula which is as shown in the specification as raw materials; and the general structural formula of the compound is as shown in the specification. The invention also discloses a method for preparing the 3,4-bi(3-indole)-2,5-dione-3-pyrrolineimine compound and application of the compound in the anti-cancer drug. According to the preparation method disclosed by the invention, the raw materials are low in price and readily available, the operation is simple, and the prepared 3,4-bi(3-indole)-2,5-dione-3-pyrrolineimine compound has high biological activity and has good application prospects in the preparation of anti-cancer drug compounds.