74556-37-9Relevant academic research and scientific papers
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
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
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.
PYRIMIDE DERIVATIVES AND THEIR PHARMACEUTICAL USE
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Page/Page column 30, (2010/04/27)
The invention provides a compound according to formula (I): wherein: X is O or S; Y is O or S; each Ar and Ar' is independently a mono-, bi- or tricyclic aryl or heteroaryl group optionally substituted with one or more substituents selected from halo, alk
Novel cambinol analogs as sirtuin inhibitors: Synthesis, biological evaluation, and rationalization of activity
Medda, Federico,Russell, Rupert J. M.,Higgins, Maureen,McCarthy, Anna R.,Campbell, Johanna,Slawin, Alexandra M. Z.,Lane, David P.,Lain, Sonia,Westwood, Nicholas J.
supporting information; experimental part, p. 2673 - 2682 (2010/01/16)
The tenovins and cambinol are two classes of sirtuin inhibitor that exhibit antitumor activity in preclinical models. This report describes modifications to the core structure of cambinol, in particular by incorporation of substitutents at the N1-position, which lead to increased potency and modified selectivity. These improvements have been rationalized using molecular modeling techniques. The expected functional selectivity in cells was also observed for both a SIRT1 and a SIRT2 selective analog.
Condensation of α-aroylketene dithioacetals and 2- hydroxyarylaldehydes results in facile synthesis of a combinatorial library of 3-aroylcoumarins
Rao, H. Surya Prakash,Sivakumar
, p. 8715 - 8723 (2007/10/03)
A facile, convenient, efficient, and high yielding synthesis of a combinatorial library of 3-aroylcoumarins has been developed by the condensation of easily available α-aroylketene dithioacetals (AKDTAs) and 2-hydroxybenzaldehydes (salicylaldehydes)/2-hydroxy-1-naphthaldehyde in the presence of catalytic amount of piperidine in THF reflux. The condensation of ferrocene derived α-aroylketene dithioacetal and 2-hydroxybenzaldehyde furnished coumarin installed on a ferrocene platform.
FIVE-MEMBERED 2,3-DIOXOHETEROCYCLES. IV. AROYLACETYLATION OF PHENOLS BY 5-ARYL-2,3-DIHYDROFURAN-2,3-DIONES
Andreichikov, Yu. S.,Tokmakova, T. N.
, p. 796 - 800 (2007/10/02)
Phenyl aroylacetates were obtained by the reaction of phenols and pyrocatechol with 5-aryl-2,3-dihydrofuran-2,3-diones under conditions for the decarbonylation of the latter.The reaction between 5-aryl-2,3-dihydrofuran-2,3-diones and salicylaldehyde and 2-hydroxynapthaldehyde under the same conditions led to the formation of 3-aroyl-2H-chromen-2-ones, 2-(2-aroylacetoxy)phenyl-6-aryl-1,3-dioxin-4-ones, and 3-aroyl-2H-benzochromen-2-ones.
