- Compounds and methods for treating tumors
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The present invention relates to pharmaceutical compositions and methods for controlling tumor growth in cancer patients. These compounds and pharmaceutical compositions modulate the P-glycoprotein multidrug transporter system and inhibit the activated PI3K/Akt/mTOR/p70S6K signaling pathway. The compounds and pharmaceutical compounds of the present invention are particularly useful for treating metastatic and drug-resistant tumors.
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Page/Page column 12
(2015/12/17)
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- Microwave-assisted phenothiazines preparation by thionation of diphenylamines
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A preparation in 'dry media' of phenothiazine derivatives by thionation of diphenylamines using microwave-activation is presented. This method allowed the preparation of 2,4,6,8-tetra-tert-butyl-10H-phenothiazine 2e, the first 2,4,6,8-tetra-substituted derivative of this heterocycle, practically inaccessible by other thionation procedure.
- Filip, Sorin V.,Silberg, Ioan A.,Surducan, Emanoil,Vlassa, Mircea,Surducan, Vasile
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p. 337 - 345
(2007/10/03)
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- Process for the direct and regioselective functionalization in position 2 of phenothiazine
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A process for the direct and regioselective functionalization of phenothiazine which allows to introduce an SH group in position 2 by reaction with sulfur dioxide (SO2) and aluminum trichloride (AlCl3) with subsequent reduction is described. The thus obtained 2-mercapto-phenothiazine is easy transformed into 2-methylthio-phenothiazine, an important intermediate for the preparation of pharmacological active compounds.
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- Process for the direct and regioselective functionalization in position 2 of phenothiazine
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Preparation of 2-alkylthio-phenothiazines by direct functionalization of phenothiazine by reaction of the phenothiazine, N-protected by an acryl group, with a sulfonating agent such as sulfuric acid, sulfuric anhydride, chlorosulfonic acid, or oleum, in order to obtain, after work-up of the reaction mixture, phenothiazine-2-sulfonic acid, followed by the reduction of this or, optionally, of its acyl chloride derivative, to obtain 2-mercapto-phenothiazine which subsequently is subjected to S-alkylation to thereby obtain the desired target compound.
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- Process for the direct and regioselective functionalization in position 2 of phenotiazine
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A process for the direct and regioselective functionalization of phenothiazine which allows to introduce an SH group in position 2 is described. The thus obtained 2-mercapto-phenothiazine is easy transformed into 2-methylthio-phenothiazine, an important intermediate for the preparation of pharmacological active compounds.
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