1032-67-3Relevant academic research and scientific papers
An environmentally benign solvent/catalyst-free one-pot synthesis of N-substituted phthalimides via Aza-wittig reaction
Sathishkumar, Murugan,Palanikumar, Kulandaivel,Mariappan, Arumugam,Archana, Sivasubramaniyan,Ponnuswamy, Alagusundaram
, p. 681 - 685 (2012)
For the first time an environmentally benign solvent/catalyst-free protocol for the synthesis of a variety of N-substituted phthalimides is submitted. It involves a one-pot coupling of nascent phosphazene generated in situ with phthalic anhydride. The protocol is novel in (1) avoiding toxic solvents, (2) no catalyst is employed and (3) no isophthalimide is formed as noted in the prevailing solution phase/catalysed methodology. Iranian Chemical Society 2012.
The preparation and in vitro antiproliferative activity of phthalimide based ketones on MDAMB-231 and SKHep-1 human carcinoma cell lines
Chan, Sau Hing,Lam, Kim Hung,Chui, Chung Hin,Gambari, Roberto,Yuen, Marcus Chun Wah,Wong, Raymond Siu Ming,Cheng, Gregory Yin Ming,Lau, Fung Yi,Au, Yiu Kwok,Cheng, Chor Hing,Lai, Paul Bo Shan,Kan, Chi Wai,Kok, Stanton Hon Lung,Tang, Johnny Cheuk On,Chan, Albert Sun Chi
, p. 2736 - 2740 (2009)
The 'one pot' condensation reaction for the synthesis and potent antiproliferative inhibition of α-phthalimide based ketones is reported here. 2-Phthalimide-1-(4-fluoro-phenyl)ethanone (5) showed the best growth inhibition on human MDAMB-231 breast carcin
Palladium-catalyzed asymmetric hydrogenation of functionalized ketones
Wang, You-Qing,Lu, Sheng-Mei,Zhou, Yong-Gui
, p. 3235 - 3238 (2005)
(Chemical Equation Presented) A novel catalytic system for asymmetric hydrogenation of functionalized ketones has been developed using a Pd/bisphosphine complex as the catalyst in 2,2,2-trifluoroethanol. The reaction exhibits high enantioselectivity, and
Ru-catalyzed asymmetric hydrogenation of α-phthalimide ketones and 1,3-diaryl diketones using 4,4′-substituted BINAPs
Hu, Aiguo,Lin, Wenbin
, p. 455 - 458 (2005)
(Chemical Equation Presented) A family of tunable precatalysts [NH 2Et2][{Ru(4,4′-BINAP)Cl}2(μ-Cl) 3] was synthesized and used for highly enantioselective hydrogenation of phthalimide-protected amino ketones and
Dual Parasiticidal Activities of Phthalimides: Synthesis and Biological Profile against Trypanosoma cruzi and Plasmodium falciparum
Teixeira de Moraes Gomes, Paulo André,Veríssimo de Oliveira Cardoso, Marcos,dos Santos, Ignes Regina,Amaro de Sousa, Fabiano,da Concei??o, Juliana Maria,Gouveia de Melo Silva, Vanessa,Duarte, Denise,Pereira, Raquel,Oliveira, Rafael,Nogueira, Fátima,Alves, Luiz Carlos,Brayner, Fabio André,da Silva Santos, Aline Caroline,Rêgo Alves Pereira, Valéria,Lima Leite, Ana Cristina
, p. 2164 - 2175 (2020)
Chagas disease and malaria are two neglected tropical diseases (NTDs) that prevail in tropical and subtropical regions in 149 countries. Chagas is also present in Europe, the US and Australia due to immigration of asymptomatic infected individuals. In the absence of an effective vaccine, the control of both diseases relies on chemotherapy. However, the emergence of parasite drug resistance is rendering currently available drugs obsolete. Hence, it is crucial to develop new molecules. Phthalimides, thiosemicarbazones, and 1,3-thiazoles have been used as scaffolds to obtain antiplasmodial and anti-Trypanosoma cruzi agents. Herein we present the synthesis of 24 phthalimido-thiosemicarbazones (3 a–x) and 14 phthalimido-thiazoles (4 a–n) and the corresponding biological activity against T. cruzi, Plasmodium falciparum, and cytotoxicity against mammalian cell lines. Some of these compounds showed potent inhibition of T. cruzi at low cytotoxic concentrations in RAW 264.7 cells. The most active compounds, 3 t (IC50=3.60 μM), 3 h (IC50=3.75 μM), and 4 j (IC50=4.48 μM), were more active than the control drug benznidazole (IC50=14.6 μM). Overall, the phthalimido-thiosemicarbazone derivatives were more potent than phthalimido-thiazole derivatives against T. cruzi. Flow cytometry assay data showed that compound 4 j was able to induce necrosis and apoptosis in trypomastigotes. Analysis by scanning electron microscopy showed that T. cruzi trypomastigote cells treated with compounds 3 h, 3 t, and 4 j at IC50 concentrations promoted changes in the shape, flagella, and surface of the parasite body similar to those observed in benznidazole-treated cells. The compounds with the highest antimalarial activity were the phthalimido-thiazoles 4 l (IC50=1.2 μM), 4 m (IC50=1.7 μM), and 4 n (IC50=2.4 μM). Together, these data revealed that phthalimido derivatives possess a dual antiparasitic profile with potential effects against T. cruzi and lead-like characteristics.
COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY
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Page/Page column 172-173, (2020/07/31)
This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.
MAP4K4 INHIBITORS
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Paragraph 00303, (2020/07/05)
This invention relates to compounds that may be useful as inhibitors of Mitogen-activated Protein Kinase Kinase Kinase Kinase-4 (MAP4K4). The invention also relates to the use of these compounds, for example in a method of treatmentof cardiac conditions.In particular, the present invention relates to compounds of formula (I):
COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY
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Page/Page column 95; 96, (2020/01/31)
This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.
MAP4K4 INHIBITORS
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Paragraph 00222, (2019/05/02)
This invention relates to pyrrolopyrimidine comprising compounds that may be useful as inhibitors of Mitogen-activated Protein Kinase Kinase Kinase Kinase-4 (MAP4K4). The invention also relates to the use of these pyrrolopyrimidine comprising compounds, f
dipyrromethene-type compound, colorant compositions comprising the same, quencher for improving of contrast ratio comprising the same and color filter comprising the same
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Paragraph 0061; 0062, (2017/04/03)
The present invention relates to a dipyrromethene-type compound. Specifically, the present invention relates to the dipyrromethene-type compound which is a dipyrromethene metal complex represented by chemical formula 1 or chemical formula 2, and dipyrrome
