- A study of the Claisen-Eschenmoser reaction for hydroxymethylbenzofurans and-indoles
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N,N-Dimethylacetamide dimethyl acetal reacted with 5(7)-substituted 2-(hydroxy-methyl)benzofurans to give N,N-dimethyl-2-(2-methylbenzofuran-3-yl) acetamides. Analogous reactions with 3-(hydroxymethyl)indole and 1-hydroxy-6-methyl-1,2,3,4-tetrahydro-carbazole afforded N,N-dimethyl-3-(3- indolyl)propionamide and N, N-dimethyl-2-(6-methyl-1,2,3,4-tetrahydrocarbazol-1- yl)acetamide, respectively.
- Mukhanova,Kukushkin,Ivanov,Alekseeva,Granik
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- PROTEIN KINASE C AGONISTS
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The present disclosure relates generally to certain diacylglycerol lactone compounds, pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions dis
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Paragraph 0341; 0342
(2020/09/12)
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- Cytotoxicity of new pyridazin-3(2H)-one derivatives orchestrating oxidative stress in human triple-negative breast cancer (MDA-MB-468)
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Triple-negative breast cancer (TNBC) is a complex and aggressive subtype of breast cancer characterized by high morbidity and mortality. In the absence of targeted therapy, only chemotherapy is available in this case of cancer. The current study investigated the antitumor effect of new pyridazin-3(2H)-one derivatives on the human TNBC cell line, MD-MB-468. The in vitro cytotoxic activities were investigated using the tetrazolium-based MTT assay. Lipid peroxidation, H2O2 content, and the specific activities of antioxidant enzymes were also determined. Two molecules, 6f and 7h, were found to be selectively highly active against tumor cells with IC50 values of 3.12 and 4.9 μM, respectively. Furthermore, cells exposed to 6f showed a significant increase in H2O2 and lipid peroxidation levels, accompanied by a decrease in the enzyme activities of glutathione reductase (GR) and thioredoxin reductase (TrxR). The cytotoxicity of the compound 6f may improve the therapeutic efficacy of the current treatment for TNBC via the inhibition of GR and TrxR activities.
- Bouchmaa, Najat,Ben Mrid, Reda,Boukharsa, Youness,Nhiri, Mohamed,Ait Mouse, Hassan,Taoufik, Jamal,Ansar, M'hammed,Zyad, Abdelmajid
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- PD-1/PD-L1 INHIBITORS
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Compounds according to formula (I), methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.
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Page/Page column 409; 410
(2018/11/22)
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- GLUCOSYLCERAMIDE SYNTHASE INHIBITORS FOR THE TREATMENT OF DISEASES
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Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).
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Paragraph 000432
(2015/04/15)
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- One-step transformation of 2- or 3-(1-hydroxyalkyl) -2,3-dihydrobenzofurans to the acylbenzofurans with N-bromosuccinimide
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The one-step transformation of 2- or 3-(1-hydroxyalkyl)-2, 3-dihydrobenzofurans (1 or 2) to the 2- or 3-acylbenzofurans (5 or 6) with N-bromosuccinimide was performed with good yields. The reaction is characterized to take place via the continuous bromina
- Suzuki, Hideaki,Tsutsui, Hideyuki,Kano, Atsuyuki,Katoh, Satoru,Morita, Tadashi,Matsuda, Kiyoshi,Iibuchi, Norihiro,Ogawa, Masashi
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p. 1657 - 1661
(2007/10/03)
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- Synthesis of 2-amino-4-(2-benzofuryl)Δ1 pyrrolines and study of their antidysrhythmic properties
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The synthesis of 2-amino 4(2-benzofuryl)Δ1 pyrrolines, substituted in the aromatic ring and/or on the nitrogen atom of the amino group, is described. These derivatives are obtained from 3 (2-benzofuryl) acrylic esters, on which nitromethane is added. The reduction of 4-nitrobutyric esters lead to pyrrolidinones, and then to the entitled derivatives. Some analogs, the benzofuran ring of which is replaced by another heterocycle, were also prepared. Some of them exhibit interesting antidysrhythmic properties.
- Maillard,Langlois,Vo Van,et al.
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p. 353 - 358
(2007/10/02)
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