4852-81-7Relevant academic research and scientific papers
Ros inhibitory activity and cytotoxicity evaluation of benzoyl, acetyl, alkyl ester, and sulfonate ester substituted coumarin derivatives
Salar, Uzma,Mohammed Khan, Khalid,Jabeen, Almas,Faheem, Aisha,Naqvi, Farwa,Ahmed, Shakil,Iqbal, Erum,Ali, Farman,Kanwal,Perveen, Shahnaz
, p. 1099 - 1111 (2020/11/09)
Background: A number of non-steroidal anti-inflammatory drugs (NSAIDs) including aspirin, indomethacin, ibuprofen, flufenamic acid, and phenylbutazone are being clinically used to treat inflammatory disorders. These NSAIDs are associated with serious side
Optical, electrochemical and current?voltage characteristics of novel coumarin based 2,4-dinitrophenylhydrazone derivatives
Arthoba Nayaka, Y.,Basavarajappa, K. V.,Manjunatha, K. B.,Purushothama, H. T.,Rudresha, B. J.,Vinay, M. M.,Yathisha, R. O.
, (2019/08/26)
A series of novel 2,4-dinitrophenylhydrazone derivatives of coumarins (DNP1?DNP3) have been synthesized by novel method and characterized by spectroscopic techniques and were used as photosensitizers on zinc nanocones, which were prepared by microwave com
COMPOSITIONS AND METHODS FOR INHIBITING N-SMASE2
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Page/Page column 29, (2019/04/11)
Provided herein are compounds of Formula (I) and (II) and their salts, and compositions comprising such compounds that are useful for useful for modulating neutral sphingomyelinase 2 (n-SMase2) in cells. Also disclosed herein are methods of using the disc
Anti-MRSA (Multidrug resistant Staphylococcus aureus) activity of 3-substituted coumarins
Salar, Uzma,Khan, Khalid Mohammed,Muhammad, Humaira,Fakhri, Muhammed Imran,Sanaullah,Perveen, Shahnaz,Choudhary, Muhammed Iqbal
, p. 353 - 362 (2018/04/20)
Background: Infectious pathogenic bacteria are the key virulence in our daily life. Especially diseases produced by multidrug resistant Staphylococcus aureus (MRSA) still contributing in morbidity and mortality in humans. Discovery of new and safer antibi
Synthesis of functionalized benzo[f]2H-chromenes and evaluation of their antimicrobial activities
Chanu, Irom Harimala,Devi, Laishram Ronibala,Khumanthem, Nonibala,Singh, N. Irabanta,Kumar, Dalip,Singh, Okram Mukherjee
, p. 177 - 185 (2017/04/24)
Knoevenagel cyclocondensations of α-hydroxy naphthaldehyde with β-oxodithioesters and ketene dithioacetals yielded 2H-benzo[f]chromene-2-thiones and 2H-benzo[f]chromen-2-ones, respectively, in high yields. The newly synthesized compounds were evaluated fo
Development of pyrazolone and isoxazol-5-one cambinol analogues as sirtuin inhibitors
Mahajan, Sumit S.,Scian, Michele,Sripathy, Smitha,Posakony, Jeff,Lao, Uyen,Loe, Taylor K.,Leko, Vid,Thalhofer, Angel,Schuler, Aaron D.,Bedalov, Antonio,Simon, Julian A.
, p. 3283 - 3294 (2014/05/20)
Sirtuins are a family of NAD+-dependent protein deacetylases that play critical roles in epigenetic regulation, stress responses, and cellular aging in eukaryotic cells. In an effort to identify small molecule inhibitors of sirtuins for potential use as chemotherapeutics as well as tools to modulate sirtuin activity, we previously identified a nonselective sirtuin inhibitor called cambinol (IC50 ≈ 50 μM for SIRT1 and SIRT2) with in vitro and in vivo antilymphoma activity. In the current study, we used saturation transfer difference (STD) NMR experiments with recombinant SIRT1 and 20 to map parts of the inhibitor that interacted with the protein. Our ongoing efforts to optimize cambinol analogues for potency and selectivity have resulted in the identification of isoform selective analogues: 17 with >7.8-fold selectivity for SIRT1, 24 with >15.4-fold selectivity for SIRT2, and 8 with 6.8- and 5.3-fold selectivity for SIRT3 versus SIRT1 and SIRT2, respectively. In vitro cytotoxicity studies with these compounds as well as EX527, a potent and selective SIRT1 inhibitor, suggest that antilymphoma activity of this compound class may be predominantly due to SIRT2 inhibition.
Biocatalytic domino reaction: Synthesis of 2H-1-benzopyran-2-one derivatives using alkaline protease from Bacillus licheniformis
Wang, Chang-Heng,Guan, Zhi,He, Yan-Hong
experimental part, p. 2048 - 2054 (2011/10/03)
A novel BLAP (alkaline protease from Bacillus licheniformis) catalyzed synthesis of 2H-1-benzopyran-2-one derivatives was achieved by domino Knoevenagel/intramolecular transesterification reaction. The control of enzymatic chemoselectivity between Knoevenagel/intramolecular transesterification and Knoevenagel/intramolecular hemiketalization could be realized by adjusting parameters including solvent, water content and temperature. The products were obtained in acceptable yields. This BLAP catalyzed selective domino reaction provided an alternative synthetic method for 2H-1-benzopyran-2-one derivatives.
Simplification of the tetracyclic SIRT1-selective inhibitor MC2141: Coumarin- and pyrimidine-based SIRT1/2 inhibitors with different selectivity profile
Rotili, Dante,Carafa, Vincenzo,Tarantino, Domenico,Botta, Giorgia,Nebbioso, Angela,Altucci, Lucia,Mai, Antonello
experimental part, p. 3659 - 3668 (2011/08/03)
In this report we describe the synthesis and biological characterization of two series of sirtuins' inhibitors (SIRTi), designed as simplification products of the previously reported SIRT1-selective inhibitor MC2141 (4). In the first series (5a-t) we report a number of 2-substituted-1,2-dihydrobenzo[f]chromen-3- ones with a marked selectivity for the inhibition of SIRT2 over SIRT1. Some of such derivatives showed also high pro-apoptotic (5i and 5l) and/or cytodifferentiating (5d, 5i, and 5o) properties in a human leukemia cell line (U937). The second group of SIRTi (6a-q) is characterized by some analogues of cambinol (3), a well known SIRTi active against the Burkitt lymphoma. Such compounds, differently from the unselective prototype, are endowed with a selective inhibition of SIRT1 over SIRT2, and, in some cases (6j, 6k, and 6q), are more efficient than 3 to induce apoptosis in U937 cells.
Synthesis and selective human monoamine oxidase inhibition of 3-carbonyl, 3-acyl, and 3-carboxyhydrazido coumarin derivatives
Secci, Daniela,Carradori, Simone,Bolasco, Adriana,Chimenti, Paola,Yá?ez, Matilde,Ortuso, Francesco,Alcaro, Stefano
experimental part, p. 4846 - 4852 (2011/11/13)
Several 3-carbonyl (1-26), 3-acyl (27-52), and 3-carboxyhydrazido (53-58) coumarins have been synthesized in high yields (72-99%) and tested in vitro for their human monoamine oxidase A and B (hMAO-A and hMAO-B) inhibitory activity. Different substituents on the coumarin nucleus were evaluated for their effect on biological activity and isoform selectivity. Substitution at position C7 of the 3-ethyl ester coumarin ring, or the introduction of a hydrazido substituent at C3, were important to obtain highly potent and selective hMAO-B inhibitors with IC50 values in the nanomolar range. Some derivatives were also submitted to a stability test and showed no chemical cleavage in vitro.
Facile synthesis of 3-thioxo-3H-benzo[f]chromen-2-yl methanone and 3H-benzo[f]chromene-3-one under solvent free condition
Singh, Okram Mukherjee,Devi, Nepram Sushuma,Devi, Laishram Ronibala,Lim, Ki Bum,Yoon, Yong Jin,Lee, Sang-Geyong
experimental part, p. 175 - 178 (2011/10/31)
A facile, convenient, efficient and high yielding synthesis of a combinatorial library of coumarins has been developed by the condensation of readily available β-oxodithioesters and S,S-acetal with 2-hydroxy-1-naphthaldehyde in the presence of catalytic a
