25244-68-2Relevant academic research and scientific papers
Photoinduced reductive repair of thymine glycol: Implications for excess electron transfer through DNA containing modified bases
Ito, Takeo,Kondo, Akiko,Terada, Satoru,Nishimoto, Sei-Ichi
, p. 10934 - 10942 (2006)
Photoinduced reduction of thymine glycol in oligodeoxynucleotides was investigated using either a reduced form of flavin adenine dinucleotide (FADH-) as an intermolecular electron donor or covalently linked phenothiazine (PTZ) as an intramolecular electron donor. Intermolecular electron donation from photoexcited flavin (*FADH-) to free thymidine glycol generated thymidine in high yield, along with a small amount of 6-hydroxy-5,6-dihydrothymidine. In the case of photoreduction of 4-mer long single-stranded oligodeoxynucleotides containing thymine glycol by *FADH-, the restoration yield of thymine was varied depending on the sequence of oligodeoxynucleotides. Time-resolved spectroscopic study on the photo-reduction by laser-excited N,N-dimethylaniline (DMA) suggested elimination of a hydroxyl ion from the radical anion of thymidine glycol with a rate constant of ～104 s-1 generates 6-hydroxy-5,6-dihydrothymidine (6-HOT?) as a key intermediate, followed by further reduction of 6-HOT? to thymidine or 6-hydroxy-5,6-dihydrothymdine (6-HOT). On the other hand, an excess electron injected into double-stranded DNA containing thymine glycol was not trapped at the lesion but was further transported along the duplex. Considering redox properties of the nucleobases and PTZ, competitive excess electron trapping at pyrimidine bases (thymine, T and cytosine, C) which leads to protonation of the radical anion (T-?, C-?) or rapid back electron transfer to the radical cation of PTZ (PTZ-?), is presumably faster than elimination of the hydroxyl ion from the radical anion of thymine glycol in DNA.
Synthesis of Novel β-Lactams from Phenothiazin-10-ylacetic Acid
Omidvari, Zahra,Zarei, Maaroof
, p. 1085 - 1091 (2018)
The first synthesis of 3-phenothiazine-β-lactams is herein reported. Thirteen new derivatives of β-lactams were synthesized using various Schiff bases and (phenothiazin-10-yl)acetic acid, which in turn was prepared starting from phenothiazine. The sole product of the Staudinger ketene–imine [2?+?2] cycloaddition reaction is the trans-β-lactam. All the synthesized compounds were characterized by elemental analyses and spectral (IR, 1H-NMR, and 13C-NMR) data.
SMALL MOLECULE INHIBITORS OF AUTOPHAGY AND HISTONE DEACTYLASES AND USES THEREOF
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, (2021/05/07)
This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a quinoline or thioxanthenone (or similar) structure which function as autophagy inhibitors and/or histone deactylase inhibitors, and their use as therapeutics for the treatment of conditions characterized with aberrant autophagy activity and/or aberrant HDAC activity (e.g., cancer, pulmonary hypertension, diabetes, neurodegenerative disorders, aging, heart disease, rheumatoid arthritis, infectious diseases, conditions and symptoms caused by a viral infection (e.g., COVID-19)).
N of a kind of preparation method of-carbencillin methyl phenothiazine
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Paragraph 0032-0060, (2019/02/02)
The invention relates to a method for preparing N-carboxymethyl phenothiazine, which comprises the following steps: directly mixing phenothiazine, potassium chloroacetate and N,N-dimethyl formamide, and heating while adjusting the pH value to 8-9; cooling the reaction liquid and adjusting to strong acidity, and adding the solution into water to obtain a product. According to the method provided by the invention, phenothiazine and potassium chloroacetate are used as raw materials, the product is synthesized by one step, the reaction time is short, the reaction process is simple, and the operation is easy; moreover, the conversion rate of the raw materials is very high, the yield of the obtained product exceeds 95%, and the new design thought provides more application space for the synthesis of N-carboxymethyl phenothiazine.
Synthesis and antioxidant evaluation of novel phenothiazine linked substitutedbenzylideneamino-1,2,4-triazole derivatives
Maddila, Suresh,Momin, Mehbub,Gorle, Sridevi,Palakondu, Lavanya,Jonnalagadda, Sreekanth B.
, (2015/11/03)
A series of novel 5-((10H-phenothiazin-10yl)methyl)-4-(substitutedbenzylideneamino)-4H-1,2,4-triazole-3-thiol derivatives (6a-i) have been synthesized from compound (1) through a multi-step reaction. The key intermediate (5) afforded a series of title com
INHIBITORS OF MALT1 PROTEASE
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, (2014/06/24)
The present invention relates to compounds which are inhibitors of mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALTl) and to their use in therapy, in particular in the treatment or prevention of a disease or disorder which is treatable by an inhibitor of a paracaspase. The present invention also relates to pharmaceutical compositions containing such compounds.
Synthesis and anti-inflammatory activity of fused 1,2,4-triazolo-[3,4-b] [1,3,4]thiadiazole derivatives of phenothiazine
Maddila,Gorle,Singh,Lavanya,Jonnalagadda
, p. 977 - 983 (2013/12/04)
A new series of 10-((6-(substitutedphenyl)-[1,2,4]triazolo[3,4-b][1,3,4] thiadiazol-3-yl)methyl)-10H-phenothiazine derivatives (7a-k) moiety was prepared using intermediate compound 5-((10H-phenothiazin-10-yl)methyl)-4-amino-4H-1,2, 4-triazole-3-thiol (5). The structures of newly synthesized compounds were confirmed on the basis of their 1H NMR, 13C NMR, LCMS mass, FT-IR and elemental analysis data results. All the compounds were screened for their significant anti-inflammatory activity of inhibition in paw oedema at 3h and 5h respectively, compared to the standard drug indomethacin. The Compounds 7k and 7d showed potent activity, while compounds 7g, 7b, 7j, 7i and 7c exhibited significant activity when compared to the standard drug, due to the presence of mild electron withdrawing groups such as difluoro, fluorine, chlorofluoro, nitro and chlorine derivatives which are attached to the benzene rings. 2013 Bentham Science Publishers.
Phenothiazine as an aromatic capping group to construct a short peptide-based 'super gelator'
Ou, Caiwen,Zhang, Jianwu,Zhang, Xiaoli,Yang, Zhimou,Chen, Minsheng
supporting information, p. 1853 - 1855 (2013/03/14)
We report a 'super-gelator' of a short peptide capped with phenothiazine acetic acid.
New farnesyltransferase inhibitors in the phenothiazine series
Belei, Dalila,Dumea, Carmen,Samson, Alexandrina,Farce, Amaury,Dubois, Joelle,Bicu, Elena,Ghinet, Alina
, p. 4517 - 4522 (2012/08/07)
The biological screening of the chemical library of our Organic Chemistry Department, carried out on an automated fluorescence-based FTase assay, allowed us to discover that a phenothiazine derivative (1d) was an inhibitor of farnesyltransferase. Three new series of human farnesyltransferase inhibitors, based on a phenothiazine scaffold, were synthesized with protein farnesyltransferase inhibition potencies in the low micromolar range. Ester derivative 9d was the most active compound in these series. Four synthesized compounds were evaluated for their antiproliferative activity on a NCI-60 cancer cell line panel. The modest results obtained in this preliminary investigation showed that mixing the phenothiazine and the 1,2,3-triazole motif in the structure of a single compound can lead to new scaffolds in the field of farnesyltransferase inhibitors.
Photolyase-like repair of psoralen-crosslinked nucleic acids
Stafforst, Thorsten,Hilvert, Donald
supporting information; experimental part, p. 9483 - 9486 (2011/11/11)
Psoralen-derived photolesions are efficiently repaired by a photolyase-like mechanism. The removal of the interstrand crosslink by photoelectron injection confers control over biochemical processes by light (see picture). This paves the way to new, site-selective uncaging applications, as demonstrated with a primer extension assay.
