40665-26-7Relevant academic research and scientific papers
Synthesis and Luminescence Spectral Properties of New Cyano-Substituted 2,2′-Bipyridine Derivatives
Bardasov, I. N.,Belikov, M. Yu.,Ershov, O. V.,Ievlev, M. Yu.,Mayorov, N. S.,Shishlikova, M. A.
, p. 1961 - 1967 (2022/01/24)
Abstract: Previously unknown 2-{4-aryl-5-cyano-[2,2′-bipyridin]-6(1H)-ylidene}malononitriles were synthe-sized by reaction of 3-aryl-1-(pyridin-2-yl)prop-2-en-1-ones (azachalcones) with malononitrile dimer. Their colored solutions showed fluorescence in t
A novel dialkylamino-functionalized chalcone, DML6, inhibits cervical cancer cell proliferation, in vitro, via induction of oxidative stress, intrinsic apoptosis and mitotic catastrophe
Chandrabose, Karthikeyan,Elangovan, Manivannan,Hari Narayana Moorthy, N. S.,Hussein, Noor,Len, Jenna M.,Malla, Saloni,McIntosh, Kyle,Pandey, Manoj,Patidar, Rahul,Raman, Dayanidhi,Tiwari, Amit K.,Trivedi, Piyush
, (2021/07/26)
In this study, we designed, synthesized and evaluated, in vitro, novel chalcone analogs containing dialkylamino pharmacophores in the cervical cancer cell line, OV2008. The compound, DML6 was selective and significantly decreased the proliferation of OV20
Design, Synthesis, and Evaluation of Chalcone Derivatives as Multifunctional Agents against Alzheimer's Disease
Wang, Xiao-Qin,Zhou, Lu-Yi,Tan, Ren-Xian,Liang, Guo-Peng,Fang, Si-Xian,Li, Wei,Xie, Mei,Wen, Yu-Hao,Wu, Jia-Qiang,Chen, Yi-Ping
, (2021/10/19)
Fifteen chalcone derivatives 3a–3o were synthesized, and evaluated as multifunctional agents against Alzheimer's disease. In vitro studies revealed that these compounds inhibited self-induced Aβ1-42 aggregation effectively ranged from 45.9–94.5
Experimental and Theoretical Studies of the Spectroscopic Properties of Chalcone Derivatives
Pietrzak, Marek,Józefowicz, Marek,Bajorek, Agnieszka,Heldt, Janina R.
, p. 537 - 549 (2017/03/07)
Newly synthesized, differently substituted chalcones (1,3-diaryl-2-propen-1-ones) have been studied using steady-state and time-resolved techniques combined with quantum-chemical modelling. To explore spectroscopic structure - property relationships the substituent (acceptor moiety) was chosen according to systematic variation in the Hammett parameter. It was shown that photophysical properties of the studied donor-acceptor (D-A) molecules can be predicted in terms of a simple model from the properties of individual chromophores (composite-model of decoupled moieties: donor (D) and acceptor (A)). The results of spectroscopic measurements also indicate that for investigated D-A fluorophores in medium-polar solvent, the initially populated, locally excited (LE) state (where the fundamental role plays donor moiety (D*-A)) reacts further to produce intramolecular charge transfer (ICT) state. Additionally, the experimental absorption (Mge) and fluorescence (Meg) transition dipole moments were calculated on the basis of spectroscopic data and compared with results of our quantum-chemical calculations. The absorption transition dipole moment was found to vary linearly with the Hammett substituent coefficient (σ).
Design, synthesis and bioactivity of chalcones and its analogues
Niu, Chao,Tuerxuntayi, Adila,Li, Gen,Kabas, Madina,Dong, Chang-Zhi,Aisa, Haji Akber
supporting information, p. 1533 - 1538 (2017/07/17)
The Vernohia anthelmintica L.'s extract is one of the most popular Uygur medicines used for vitiligo. It is believed that the chalcone compounds of the plant play an important role in the treatment since they may activate tyrosinase and improve melanin production. In this study, twenty-one chalcones and nine analogues were synthesized in view of three different components of chalcone (A, B ring and α, β-unsaturated carbonyl). After biological evaluation of their activity on tyrosinase in cell-free systems, the result showed that most compounds (except polyhydroxy chalcones) possess activator effect on the tyrosinase, especially for 13a–15a, 20a and 1b, which bearing a comparable activity to the positive control 8-MOP. SAR of these tyrosinase activator was summed up for the first time as well. Finally, compound 13a was found to increase melanin contents and tyrosinase activity 1.75 and 1.3 fold, respectively, compared with that of untreated murine B16 cells at the concentration of 40?μg/mL.
Inhibitory Kinetics of Azachalcones and their Oximes on Mushroom Tyrosinase: A Facile Solid-state Synthesis
Radhakrishnan, Sini K.,Shimmon, Ronald G.,Conn, Costa,Baker, Anthony T.
, p. 531 - 538 (2016/06/01)
A solid-state-based mechanochemical process was used to synthesize novel azachalcones and their oximes as tyrosinase inhibitors. Their inhibitory activities on mushroom tyrosinase using l-3,4-dihydroxyphenylalanine as a substrate were investigated. Two of
The synthesis and structures of arene-substituted azadipyrromethenes
Chanawanno, Kullapa,Hasheminasab, Abed,Engle, James T.,Ziegler, Christopher J.
, p. 276 - 281 (2015/10/19)
We present the synthesis of several azadipyrromethenes with four peripheral arene units which can be readily generated via the well-established chalcone synthetic method. The stability and yields of these azadipyrromethenes is highly dependent on the nature of the arene substituent, with the bis-pyridine systems exhibiting the highest degree of instability. The structures of several of the compounds and their BF2 adducts are presented; intramolecular hydrogen bonding is observed in the free base ADPMs. We also present a study into the absorption and emission properties of the ADPMs and their BF2 adducts and observe that they are also highly dependent on the identity of the substituents.
Effects of structural modifications on the metal binding, anti-amyloid activity, and cholinesterase inhibitory activity of chalcones
Fosso, Marina Y.,LeVine, Harry,Green, Keith D.,Tsodikov, Oleg V.,Garneau-Tsodikova, Sylvie
, p. 9418 - 9426 (2015/09/15)
As the number of individuals affected with Alzheimer's disease (AD) increases and the availability of drugs for AD treatment remains limited, the need to develop effective therapeutics for AD becomes more and more pressing. Strategies currently pursued include inhibiting acetylcholinesterase (AChE) and targeting amyloid-β (Aβ) peptides and metal-Aβ complexes. This work presents the design, synthesis, and biochemical evaluation of a series of chalcones, and assesses the relationship between their structures and their ability to bind metal ions and/or Aβ species, and inhibit AChE/BChE activity. Several chalcones were found to exhibit potent disaggregation of pre-formed N-biotinyl Aβ1-42 (bioAβ42) aggregates in vitro in the absence and presence of Cu2+/Zn2+, while others were effective at inhibiting the action of AChE.
Spectral studies of 2-pyrazoline derivatives: Structural elucidation through single crystal XRD and DFT calculations
Chinnaraja,Rajalakshmi,Srinivasan,Velmurugan,Jayabharathi
supporting information, p. 30 - 33 (2014/02/14)
A series of biologically active N-thiocarbamoyl pyrazoline derivatives have been synthesized using anhydrous potassium carbonate as the catalyst. All the synthesized compounds were characterized by FT-IR, 1H NMR, 13C NMR spectral stu
Synthesis, pharmacological and biological screening of some novel pyrimidine derivatives
Ishwar Bhat,Kumar, Abhishek,Nisar, Muhammed,Kumar, Pankaj
, p. 3458 - 3467 (2014/06/24)
In the present study a new series of 4-substituted phenyl-6-(pyridin-2-yl) pyrimidin-2-ol (1-9) and 4-substituted phenyl-6-(pyridin-2-yl)pyrimidin-2-thiol (10-18) have been synthesized by cyclizing 3-substituted phenyl-1-(pyridin-2-yl) prop-2-en-1-one wit
