1020399-36-3Relevant academic research and scientific papers
1,5-Diphenyl-1,4-pentadiene-3-ones and cyclic analogues as antioxidative agents. Synthesis and structure-activity relationship
Sardjiman,Reksohadiprodjo,Hakim,Van Der Goot,Timmerman
, p. 625 - 630 (1997)
A series of 1,5-diphenyl-1,4-pentadiene-3-ones and cyclic analogues with OH-groups in the para position of the phenyl rings and various meta substituents were prepared and their antioxidant activity compared with that of curcumin. Most of them exhibited potent antioxidative activity, especially when all the meta positions were substituted by methoxy groups.
Epigenetic multiple ligands: Mixed histone/protein methyltransferase, acetyltransferase, and class III deacetylase (Sirtuin) inhibitors
Mai, Antonello,Cheng, Donghang,Bedford, Mark T.,Valente, Sergio,Nebbioso, Angela,Perrone, Andrea,Brosch, Gerald,Sbardella, Gianluca,De Bellis, Floriana,Miceli, Marco,Altucci, Lucia
, p. 2279 - 2290 (2008/12/22)
A number of new compounds bearing two ortho-bromo- and ortho,ortho- dibromophenol moieties linked through a saturated/unsaturated, linear/(poly)cyclic spacer (compounds 1-9) were prepared as simplified analogues of AMI-5 (eosin), a recently reported inhibitor of both protein arginine and histone lysine methyltransferases (PRMTs and HKMTs). Such compounds were tested against a panel of PRMTs (RmtA, PRMT1, and CARM1) and against human SET7 (a HKMT), using histone and nonhistone proteins as a substrate. They were also screened against HAT and SIRTs, because they are structurally related to some HAT and/or SIRT modulators. From the inhibitory data, some of tested compounds (1b, 1c, 4b, 4f, 4j, 4l, 7b, and 7f) were able to inhibit PRMTs, HKMT, HAT, and SIRTs with similar potency, thus behaving as multiple ligands for these epigenetic targets (epi-MLs). When tested on the human leukemia U937 cell line, the epi-MLs induced high apoptosis levels [i.e., 40.7% (4l) and 42.6% (7b)] and/or massive, dose-dependent cytodifferentiation [i.e., 95.2% (1c) and 96.1% (4j)], whereas the single-target inhibitors eosin, curcumin, and sirtinol were ineffective or showed a weak effect.
Synthesis of Curcumin Analogues as Potential Antioxidant, Cancer Chemopreventive Agents
Youssef, Khairia M.,El-Sherbeny, Magda A.,El-Shafie, Faiza S.,Farag, Hassan A.,Al-Deeb, Omar A.,Awadalla, Sit Albanat A.
, p. 42 - 54 (2007/10/03)
New series of 3,5-bis(substituted benzylidene)-4-piperidones, 2,7-bis(substituted benzylidene)cycloheptanones, 1,5-bis(substituted phenyl)-1,4-pentadien-3-ones, 1,7-bis(substituted phenyl)-1,6-heptadien-3,5-diones, 1,1-bis(substituted cinnamoyl)-cyclopentanes, and 1,1-bis(substituted cinnamoyl)cyclohexanes have been synthesized and tested for their antioxidant activity. Among the tested compounds, compounds II 4, II9 II10, II11, V1, and V4 exhibited higher free radical scavenger activity with % inhibition values of 90.71, 91.24, 96.91, 94.26, 99.23, and 99.85%, respectively. Moreover, compound V1 is the safest member toward peripheral multinuclear neutrophils (PMNs) with a % viability value of 91%. Detailed synthesis, spectroscopic, and biological data are reported.
