Primary aminomethyl derivatives of kaempferol: hydrogen bond-assisted synthesis, anticancer activity and spectral properties

2018 ◽  
Vol 16 (11) ◽  
pp. 1921-1931
Author(s):  
Shuanglian Cai ◽  
Yangyang Kong ◽  
Dan Xiao ◽  
Yun Chen ◽  
Qiuan Wang

Primary aminomethyl derivatives of kaempferol with anticancer activity were synthesized by a combination strategy involving a hydrogen bond-assisted process.

2019 ◽  
Vol 19 (13) ◽  
pp. 1093-1110 ◽  
Author(s):  
Adel A.H. Abdel Rahman ◽  
Ibrahim F. Nassar ◽  
Amira K.F. Shaban ◽  
Dina S. EL-Kady ◽  
Hanem M. Awad ◽  
...  

Background & Objective:New diaryl-substituted pyrimidinedione compounds, their thioxo derivatives as well as their bicyclic thiazole compounds were synthesized and characterized.Methods:The glycosylamino derivatives of the synthesized disubstituted derivatives of the pyrimidine scaffold were also prepared via reaction of the N3-amino derivatives with a number of monosaccharides followed by acetylation.Results:The anticancer activity of the synthesized compounds was studied against human liver cancer (HepG2) and RPE-1cell lines. Compounds 2a, 2b, 3a and 12 showed potent activities with IC50 results comparable to that of doxorubicin.Conclusion:Docking investigations into Cyclin-dependent kinase 2 (CDK-2) enzyme, a potential target for cancer medication, were also reported showing the possible binding interaction into the enzyme active site to support their activity behavior.


2012 ◽  
Vol 9 (6) ◽  
pp. 633-637 ◽  
Author(s):  
Tomasz Plech ◽  
Monika Wujec ◽  
Urszula Kosikowska ◽  
Anna Malm ◽  
Magdalena Barylka ◽  
...  

1993 ◽  
Vol 58 (10) ◽  
pp. 2337-2348 ◽  
Author(s):  
Ivan Kmínek ◽  
Stanislav Nešpůrek ◽  
Eduard Brynda ◽  
Jiří Pfleger ◽  
Věra Cimrová ◽  
...  

The attachment of long wavelength absorbing π-conjugated chromophores to poly(methyl-phenylsilylene) (PMPSi) via reactions of its formylated derivative is described. Some of the obtained polymers exhibit improved photostability in comparison with the parent polymer. Their spectral properties and photoconductivity are discussed. Ultrathin layers and multilayers were prepared from polar derivatives of PMPSi by the Langmuir-Blodgett technique and their photoconductive behaviour was studied.


ChemInform ◽  
2010 ◽  
Vol 28 (20) ◽  
pp. no-no
Author(s):  
M. M. MOVSUMZADE ◽  
N. A. NOVRUZOVA ◽  
SH. R. ALIEV

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 1028
Author(s):  
Monnaya Chalermnon ◽  
Sarocha Cherdchom ◽  
Amornpun Sereemaspun ◽  
Rojrit Rojanathanes ◽  
Tanatorn Khotavivattana

Twelve derivatives of biguanide-derived 1,3,5-triazines, a promising class of anticancer agent, were synthesised and evaluated for their anticancer activity against two colorectal cancer cell lines—HCT116 and SW620. 2c and 3c which are the derivatives containing o-hydroxyphenyl substituents exhibited the highest activity with IC50 against both cell lines in the range of 20–27 µM, which is comparable to the IC50 of cisplatin reference. Moreover, the potential use of the calcium citrate nanoparticles (CaCit NPs) as a platform for drug delivery system was studied on a selected 1,3,5-triazine derivative 2a. Condition optimisation revealed that the source of citrate ions and reaction time significantly influence the morphology, size and %drug loading of the particles. With the optimised conditions, “CaCit-2a NPs” were successfully synthesised with the size of 148 ± 23 nm and %drug loading of up to 16.3%. Furthermore, it was found that the release of 2a from the synthesised CaCit-2a NPs is pH-responsive, and 2a could be control released under the acidic cancer environment. The knowledge from this study is perceptive for further development of the 1,3,5-triazine-based anticancer drugs and provide the platform for the incorporation of other drugs in the CaCit NPs in the future.


2017 ◽  
Vol 46 (21) ◽  
pp. 7005-7019 ◽  
Author(s):  
Benjamin W. J. Harper ◽  
Emanuele Petruzzella ◽  
Roman Sirota ◽  
Fernanda Fabiola Faccioli ◽  
Janice R. Aldrich-Wright ◽  
...  

Synthesis and biological evaluation in vitro and in vivo of functionalized Pt(iv) derivatives of Pt56MeSS.


1979 ◽  
Vol 10 (29) ◽  
Author(s):  
A. N. GRINEV ◽  
N. V. ARKHANGEL'SKAYA ◽  
G. YA. URETSKAYA ◽  
A. A. STOLYARCHUK ◽  
P. A. GALENKO-YAROSHEVSKII

2011 ◽  
Vol 222 ◽  
pp. 271-274 ◽  
Author(s):  
Elmars Zarins ◽  
Janis Jubels ◽  
Valdis Kokars

New organic glassy non symmetric styryl- derivatives of 2(2,6-substituted-4H-pyran-4-ylidene)-malononitrile, 2(2,6-substituted-4H-pyran-4-ylidene)-1H-indene-1,3(2H)-dione and 2(2,6-substituted-4H-pyran-4-ylidene)-pyrimidine-2,4,6(1H,3H,5H)-trione were synthesized. They form thin solid amorphous films from volatile organic solvents (DCM and chloroform). Their spectral properties have been studied.


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