19152-38-6Relevant articles and documents
Synthesis and antidyslipidemic activity of chalcone fibrates
Shukla, Poonam,Srivastava, Swayam P.,Srivastava, Rohit,Rawat, Arun K.,Srivastava, Arvind K.,Pratap, Ram
, p. 3475 - 3478 (2011)
A series of chalcone based PPAR-α agonists were synthesized and evaluated for their antidyslipidemic activity in high fructose high fat fed dyslipidemic Syrian golden hamsters. Most of the compounds exhibited antidyslipidemic activity. The compounds 4c an
Synthesis, characterization, antimicrobial activities, and structural studies of Lanthanide (III) complexes with 1-(4-Chlorophenyl)-3-(4-fluoro/ hydroxyphenyl)prop-2-en-1-thiosemicarbazone
Oza, Chandra K.,Jain, Meenakshi,Jain, Neelima,Verma, Dinesh
, p. 377 - 386 (2010)
Twelve coordinate lanthanide (III) complexes with the general composition [Ln L3Xn(H2O)n] where Ln = Pr(III), Sm(III), Eu (III), Gd (III), Tb (III), Dy (III), X = Cl-1, NO3 -2, n = 2-7, and
Charge transfer based "turn-on" chemosensor for Zn2 + ion recognition using new triaryl pyrazoline derivative
Jeyanthi, Dharmaraj,Iniya, Murugan,Krishnaveni, Karuppiah,Chellappa, Duraisamy
, p. 231 - 237 (2016)
The fluoroionophore PY serves as a selective and fluorimetric chemosensor for Zn2 + based on charge transfer (CT). A mechanism for the binding mode was proposed based on fluorescence changes, NMR experiments and theoretical calculations. The 1:
Synthesis, Crystal Structure, Biological Evaluation, DFT Calculations and Third Order Nonlinear Optical Studies of Pyrazolines
Gaonkar, Santosh L.,Hari, Gangadhar,Lokanath, N. K.,Naraharisetty, Sri Ram G,Nayak, Swarnagowri,Pai, K. S. R.,Parol, Vinay,Sinha, Rajeev K.
, (2021/06/15)
Novel pyrazoline derivatives were synthesized and characterized by FTIR, NMR, UV-visible, and mass spectral studies. All the synthesized compounds 6a-f were screened for anticancer activity against MCF-7 and HCT 116 cell lines via SRB assay. Among the synthesized pyrazolines 6b and 6f showed appreciable anticancer activity. The molecular docking study was done with two proteins (PDB No: 1M17 and 5ZTO) to study the binding interactions of the compounds with proteins. ADME study showed that the compounds exhibited drug-likeness properties, following Lipinski's rule of five. The molecular structure of compound 6b was studied using the single-crystal X-ray diffraction method. The structural, absorption and first static hyperpolarizability properties of the compound 6b were studied using density functional theory (DFT) calculations. The experimental data and calculated FTIR and UV-visible spectral data are in good agreement. The third order nonlinear optical properties were studied using open and closed aperture z-scan techniques. The compound 6b showed nonlinear absorption(β) of 1.94×10?11m/W at intensity (I0) is 4.49GW/cm2. Third order nonlinear susceptibility is of the order of 10?12 esu and this indicates the molecule has the potential to be used in nonlinear optical device applications.
Chloro and bromo-pyrazole curcumin Knoevenagel condensates augmented anticancer activity against human cervical cancer cells: design, synthesis, in silico docking and in vitro cytotoxicity analysis
Chaudhary, Monika,Kumar, Neeraj,Baldi, Ashish,Chandra, Ramesh,Arockia Babu,Madan, Jitender
, p. 200 - 218 (2019/03/08)
With an endeavor to develop novel curcumin analogs as potential anti-cancer agents, we designed and synthesized a series of Knoevenagel condensates by clubbing pyrazole carbaldehydes at the active methylene carbon atom of the curcumin backbone. Molecular docking studies were carried out to target the proposed derivatives on human kinase β (IKKβ), a potential anti-cancer target. The chloro derivative displayed five hydrogen bond interactions with a docking score of ?11.874 kcal/mol higher than curcumin (docking score = ?7.434 kcal/mol). This was supported by the fact that the propellant shaped derivatives fitted aptly into the binding pocket. Molecular simulations studies were also conducted on the lead molecule and the results figured out that the stable complexes were developed as the minimal deviations per residue of protein within the range of 0.11–0.92 ?. The screened compounds were synthesized, characterized and evaluated in vitro for cytotoxicity against cervical cancer cell line, HeLa using standard cell proliferation assay. Chloro derivative and bromo analog demonstrated IC50 (half maximal inhibitory concentration) value of 14.2 and 18.6 μg/ml, respectively, significantly lower than 42.4 μg/ml of curcumin and higher than 0.008 μg/ml of paclitaxel. Induction of apoptosis was evaluated in the terms of cleavage of caspase-3 enzyme and they also exhibited 69.6 and 65.4% of apoptosis significantly higher than 19.9% induced by curcumin. In conclusion, chloro and bromo derivatives must be evaluated under a set of stringent in vitro and in vivo parameters for translating in to a clinically viable product. Communicated by Ramaswamy H. Sarma.
