114991-17-2Relevant academic research and scientific papers
Structural analysis of phenothiazine derivatives as allosteric inhibitors of the MALT1 paracaspase
Schlauderer, Florian,Lammens, Katja,Nagel, Daniel,Vincendeau, Michelle,Eitelhuber, Andrea C.,Verhelst, Steven H. L.,Kling, Dale,Chrusciel, Al,Ruland, Juergen,Krappmann, Daniel,Hopfner, Karl-Peter
, p. 10384 - 10387 (2013)
Second site: In the crystal structure of human MALT1casp-Ig3 (mucosa-associated lymphoid tissue lymphoma translocation protein 1) in complex with the tricyclic phenothiazine derivative thioridazine (violet in the picture), the inhibitor is bound in a hydrophobic pocket far from the active site. This explains the action of phenothiazine derivatives as noncompetitive, reversible inhibitors. Copyright
THIORIDAZINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF CANCER
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Page/Page column 10-12, (2021/03/13)
The present invention relates to novel thioridazine analogue compounds of formula (I): wherein R1 is OCH3 or NH2 , particularly suitable to be used in the treatment of pediatric acute myeloid leukemia harboring the t(6;11)(q27;q23) KMT2A/AFDN rearrangement.
The phenothiazine compound and its preparation method and application
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Paragraph 0109; 0110; 0112; 0113, (2018/07/30)
The invention relates to a phenothiazine compound and a preparation method thereof. The invention further relates the application of the phenothiazine compound in anti-cancer drug preparation and anti-cancer drugs using the compound as the effective component. The phenothiazine compound has the advantages that the compound with broad-spectrum anti-cancer effect is obtained by modifying phenothiazine ternary interlink parent nucleuses, synthesizing method is simple, and high yield is achieved; the phenothiazine compound has certain restraining effect on human breast cancer cells line MCF-7 and human hepatoma cell line Hep-G2, and a new thought is provided to new drugs satisfying clinic requirements.
Synthesis and SAR evaluation of novel thioridazine derivatives active against drug-resistant tuberculosis
Scalacci, Nicolò,Brown, Alistair K.,Pavan, Fernando R.,Ribeiro, Camila M.,Manetti, Fabrizio,Bhakta, Sanjib,Maitra, Arundhati,Smith, Darren L.,Petricci, Elena,Castagnolo, Daniele
, p. 147 - 158 (2016/12/30)
The neuroleptic drug thioridazine has been recently repositioned as possible anti-tubercular drug. Thioridazine showed anti-tubercular activity against drug resistant mycobacteria but it is endowed with adverse side effects. A small library of thioridazine derivatives has been designed through the replacement of the piperidine and phenothiazine moieties, with the aim to improve the anti-tubercular activity and to reduce the cytotoxic effects. Among the resulting compounds, the indole derivative 12e showed an antimycobacterial activity significantly better than thioridazine and a cytotoxicity 15-fold lower.
THE (S)-ENANTIOMER OF MEPAZINE
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, (2015/01/16)
The present invention relates to the (S)-enantiomer of mepazine, its applicability in therapy, a pharmacological composition comprising (S)-mepazine, and processes for the preparation of (S)- mepazine and one of its intermediates.
