113963-68-1Relevant articles and documents
Synthesis and cytotoxic activities of a series of novel N -methyl-bisindolylmaleimide amide derivatives
Wang, Ke,Liu, Zhan-Zhu
, p. 296 - 303 (2014)
A novel series of N-methyl-bisindolylmaleimides were synthesized and evaluated for their inhibitory activities against nine tumor cell lines. Some of the compounds showed an interesting activity against the tested cell lines. The most potent compounds 5e
New synthesis of KT5823 indolocarbazole aglycone
Burtin, Guillaume E.,Madge, David J.,Selwood, David L.
, p. 2119 - 2122 (2000)
The indolo[2,3-α]pyrrolo[3,4-c]carbazole aglycone of the selective protein kinase G inhibitor KT5823 has been synthesised in four steps and 36percent overall yield from 2,3-dichloro-N-methylmaleimide by utilising an efficient new two step reduction sequen
Friedel-Crafts alkylation on indolocarbazoles catalyzed by two dimethylallyltryptophan synthases from Aspergillus
Yu, Xia,Yang, Aigang,Lin, Wenhan,Li, Shu-Ming
, p. 6861 - 6864 (2012)
Prenylated indolocarbazoles have been reported neither from natural sources, nor by chemical synthetic approaches. In this Letter, we report a regiospecific prenylation of indolocarbazoles at the para-position of the indole N-atom by two recombinant enzymes from the dimethylallyltryptophan synthase (DMATS) superfamily, that is, 5-DMATS from Aspergillus clavatus and FgaPT2 from Aspergillus fumigatus.
Synthesis, and cytotoxic activity of Nind-alkoxy derivatives of antibiotic arcyriarubin and dechloro-rebeccamycin aglycon
Lakatosh,Balzarini,Andrei,Snoeck,De Clercq,Preobrazhenskaya
, p. 768 - 773 (2002)
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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.
With anticancer activity of 3, 4 - b (3 - indole) - 2, 5 - dione - 1 - pyrrole thiourea compound and its preparation method and application
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Paragraph 0043; 0044; 0045; 0046; 0047; 0048; 0049; 0050, (2017/08/25)
The invention discloses a 3,4-bi(3-benzpyrole)-2,5-dione-1-pyrroleimine thiourea compound with antitumor activity and a preparation method and application thereof. The technical scheme of the invention is characterized in that the 3,4-bi(3-benzpyrole)-2,5-dione-1-pyrroleimine thiourea compound with antitumor activity is prepared by taking a substituted isothiocyanate compound R-NCS and 1-amino-3,4-bi(3-benzpyrole)-3-pyrroline-2,5-dione shown in the specification as raw materials, and the structural general formula is shown in the specification. The invention further discloses the preparation method and the antitumor activity of the 3,4-bi(3-benzpyrole)-2,5-dione-1-pyrroleimine thiourea compound with antitumor activity. The preparation method disclosed by the invention has the advantages that the raw material is low in price and easily available, the operation is simple, and the prepared 3,4-bi(3-benzpyrole)-2,5-dione-1-pyrroleimine thiourea compound has better biological activity, and has better application prospect in preparation of antitumor medical compounds.