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1 Introduction
Chalcones 1,3-diphenyl-2-propen-1-ones , are based on two aryl moieties bridged via
an alpha,beta- unsaturated carbonyl group. These molecules have a -C=O-CH=CH-
ketoethylenic moiety in their structure, in their aromatic rings, they have a delocalized
pi-electron- containing order
E
D
F
Chalcone bearing Pyridine : imidazo-pyridine derivatives through the condensation of
aryl methyl ketone and aryl aldehyde in the presence of alcoholic alkali media [3] The
synthesis mixture of pyridine-3-carbaldehyde G and ethenone H was refluxed in
methanol, followed by the addition of NaOH as a catalyst. The crude was poured on
to crushed ice, and the resulting product was further recrystallized from
dichloromethane to give compound I.
I
H G
J
K
L
Chalcone Bearing Benzimidazole : A series of benzimidazole-based chalcone
derivatives were synthesized and reported using the Claisen–Schmidt reaction as
potential Topo II-targeting anticancer agents [5] . Benzimidazole derivative N was
obtained through refluxing o-phenylenediamine M with glycolic acid in the presence
of HCl. The substituted benzimidazole-2-methanol O was synthesized through the
alkylation of compound N using a benzyl bromide in the presence of K 2CO3.
Subsequently, substituted benzimidazole-2-carbaldehyde derivatives P were obtained
from O through oxidation using a Dess–Martin protocol. Compounds O were finally
prepared from P through a Claisen–Schmidt reaction in the presence of appropriate
acetophenone derivatives.
M N O
References
[1]. Özdemir, A.; Altıntop, M. D.; Sever, B.; Gençer, H. C.; Kapkaç,H. A.; Atlı, Ö.;
Baysal, M. A new series of pyrrole-based chalcones:synthesis and evaluation of
antimicrobial activity, cytotoxicity, and genotoxicity. Molecules. 2017, 22 (12), 2112.
[2] .Liu, Y. T.; Sun, X. M.; Yin, D. W.; Yuan, F. Syntheses and biological activity of
chalcones-imidazole derivatives. Res. Chem.Intermed. 2013, 39 (3), 1037−1048.
[3] .Farghaly, T. A.; Masaret, G. S.; Muhammad, Z. A.; Harras, M. F. Discovery of
thiazole-based-chalcones and 4-hetarylthiazoles as potent anticancer agents:
Synthesis, docking study and anticancer activity. Bioorganic chemistry 2020, 98,
103761
[4] . Ahmed, M. F.; Santali, E. Y.; El-Haggar, R. Novel piperazine− chalcone hybrids
and related pyrazoline analogues targeting VEGFR-2 kinase; design, synthesis,
molecular docking studies, and anticancer evaluation. Journal of enzyme inhibition
and medicinal chemistry 2021, 36 (1), 308−319.
[5] . Zhou, W.; Zhang, W.; Peng, Y.; Jiang, Z. H.; Zhang, L.; Du, Z. Design, synthesis
and anti-tumor activity of novel benzimidazole- chalcone hybrids as non-intercalative
topoisomerase II catalytic inhibitors. Molecules. 2020, 25 (14), 3180.
[6].Thirumurugan, C.; Vadivel, P.; Lalitha, A.; Lakshmanan, S.Synthesis,
characterization of novel quinoline-2-carboxamide based chalcone derivatives and
their molecular docking, photochemical studies. Synth. Commun. 2020, 50 (6),
831−839.