- In vitro and in silico growth inhibitory, anti-ovarian & anti-lung carcinoma effects of 1,5 diarylpenta-1,4-dien-3-one as synthetically modified curcumin analogue
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The synthesized 1,5 diarylpenta-1,4-dien-3-one derivatives (compounds 1-6) as synthetic curcumin analogues were tested for their potential anticancer activity against human ovarian and lung adenocarcinoma cells. The absorption, distribution, metabolism, excretion, and toxicity (ADMET/pharmacokinetic) parameters of all the compounds were predicted by admetSAR software. The pharmacokinetics, pharmacodynamics and bioactivity scores properties based on Lipinski rule and Ghose filter, calculated with the help of Molinspiration and ChemDraw. Molecular docking evaluation of all the compounds was also performed by using AutoDock Vina and iGEMDOCK against three most common human anticancer targets; epidermal growth factor receptor (EGFR), heat shock protein (Hsp 90-α), and vascular endothelial growth factor receptor-2 (VEGFR2). The obtained results were compared with the reference compound 7 and drugs 8-10 (7: GO-035; 8: Quinazolin; 9: Naquotinib and 10: Ribofuranuronamide). Finding indicates, all the compounds were potentially interacting with VEGFR2 through the average –9.1 binding energy (BE) with closer contact 1H-NMR). In vitro anti-proliferative activity was tested via MTT method against human ovarian carcinoma (PA-1) and human lung adenocarcinoma (A549) cells and further screened for apoptotic parameters such as nuclear fragmentation and ROS generation. Compound 4 exhibits good dose-dependent anti-proliferative activity (IC50 73 and 79.7 μM) against human ovarian carcinoma and human lung adenocarcinoma, respectively. Communicated by Ramaswamy H. Sarma.
- Chowrasia, Deepak,Jafri, Asif,Azad, Iqbal,Rais, Juhi,Sharma, Nisha,Khan, Fahad,Kumar, Ajay,Kumar, Sudhir,Arshad, Md
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- Stereo- and regioselective photocycloaddition of extended alkenes using γ-cyclodextrin
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Photoexcitation of dibenzalacetones (1a-d) in homogeneous media and solid state yields a mixture of products with poor conversions. Irradiation of the reactants complexed to γ-cyclodextrin predominantly affords a single dimer (syn adduct 6) despite the possibility for several monomeric and dimeric products. High selectivity in the cavitand-mediated reaction along with the structural characterization of the inclusion complex provides insight into the supramolecular interactions that drive the self-assembly of the host-guest system.
- Kashyap, Akshay,Bokosike, Treyvon K.,Bhuvanesh, Nattamai,Pattabiraman, Mahesh
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supporting information
p. 6870 - 6875
(2018/10/17)
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- Sulfamic acid: An efficient, cost-effective and green catalyst for crossed-aldol condensation of ketones with aromatic aldehydes under solvent-free
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Aromatic aldehydes undergo crossed-aldol condensation with ketones in the presence of catalytic amount of sulfamic acid (SA) to afford the corresponding α, β-unsaturated aldol products under solvent-free conditions in good to high yields at 45-80 °C.
- Rostami, Amin,Ahmad-Jangi, Firoz
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experimental part
p. 1029 - 1032
(2012/06/01)
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- Study of substituent effects in substituted dibenzal acetones
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The present work involves a detailed study of the ultra-violet absorption spectra of various substituted dibenzylidene ketones derived from acetone, ethyl methyl ketone, diethyl ketone, cyclopentanone and cyclohexanone by condensing with several meta- and para-substituted benzaldehydes in n-hexane and in ethanol to ascertain the transition dominant in these solvents. These ketones exist as equilibrium mixtures of s-cis, cis and s-cis, trans conformations. The ultraviolet absorption spectra of the ketones exhibit two bands due to π* ← π transition around 250 and 320 nm. The 320 nm band is prominent in all the cases. There is no indication of π* ← n transition in any of the spectra. The 320 nm band is structureless in all the cases except those shown by the dibenzylidene ketones derived from cyclopentanone in hexane. Therefore it can be inferred that the dibenzylide ketones derived from all the ketones except those derived from cyclopentanone are non-planar.
- Ananthakrishna Nadar,Renuga
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p. 1219 - 1222
(2008/09/21)
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- Curcumin analogs with anti-tumor and anti-angiogenic properties
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The present invention is directed to curcumin analogs exhibiting anti-tumor and anti-angiogenic properties, pharmaceutical formulations including such compounds and methods of using such compounds.
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