Synthesis and selected immunological properties of 10-substituted 1,8-diazaphenothiazines.

Medicinal Chemistry Research : an International Journal for Rapid Communications on Design and Mechanisms of Action of Biologically Active Agents
Beata Morak-MłodawskaMaja Kocięba

Abstract

A new type of tricyclic azaphenothiazines-1,8-diazaphenothiazines-was obtained in the reaction of 2,3- and 3,4-disubstituted pyridines. The reaction ran as the Smiles rearrangement. The 1,8-diazaphenothiazine system was determined using NOE experiment and 2D NMR spectra (COSY, HSQC, HMBC). 10H-1,8-diazaphenothiazine was transformed into 10-derivatives with alkyl, aminoalkyl, amidoalkyl, sulfonamidoalkyl, and nitrogen half-mustard groups. The compounds were tested for their effects on phytohemagglutinin A-induced proliferative response of human peripheral blood mononuclear cells (PBMC) and lipopolysaccharide-induced tumor necrosis factor alpha production by human whole blood cultures. The compounds exhibited differential, dose-dependent inhibitory activities in these tests. All the compounds were low toxic against PBMC. The compounds showing the highest antiproliferative activity strongly inhibited the growth of leukemia L-1210 and colon cancer SW-948 cell lines, similarly as cisplatin, a reference drug.

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Citations

Sep 30, 2016·Journal of Enzyme Inhibition and Medicinal Chemistry·Beata Morak-MłodawskaDariusz Kuśmierz
Mar 8, 2016·Journal of Enzyme Inhibition and Medicinal Chemistry·Beata Morak-MłodawskaDariusz Kuśmierz
Nov 8, 2016·Medicinal Chemistry Research : an International Journal for Rapid Communications on Design and Mechanisms of Action of Biologically Active Agents·Beata Morak-MłodawskaMałgorzata Jeleń
Sep 16, 2016·International Immunopharmacology·Jolanta ArtymKrystian Pluta
Feb 10, 2018·Journal of Chromatographic Science·Beata Morak-MlodawskaMalgorzata Jelen
Jul 17, 2019·Journal of Enzyme Inhibition and Medicinal Chemistry·Beata Morak-MłodawskaMagdalena Jurzak
Dec 6, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Beata Morak-MłodawskaDariusz Kuśmierz
Jun 7, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Jakub JończykBarbara Malawska
Sep 27, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Leon StrzadalaWojciech Kalas
Jan 16, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Beata Morak-MłodawskaDariusz Kuśmierz
Apr 4, 2021·Life·Beata Morak-MłodawskaKrystian Pluta
Apr 21, 2018·International Immunopharmacology·Jolanta ArtymJan Kuryszko
Aug 29, 2021·Medicinal Research Reviews·Kritika LaxmikeshavNagula Shankaraiah

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Methods Mentioned

BETA
X-ray
NMR
column chromatography
column

Software Mentioned

STATISTICA

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