Heteroaryl chalcones: Mini review about their therapeutic voyage

Mathew, Bijo; Suresh, Jerad; Anbazghagan, Sockalingam; Paulraj, Jayaraj; Krishnan, Girish K.

doi:10.1016/j.bionut.2014.04.003

Cited by 60 publications

(33 citation statements)

References 49 publications

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“…[5][6][7][8][9][10] Additionally to chalcones, several studies have been reported about the heterocyclic chalcones due to their pharmacological activities, which are attributed to the structural aspects of these molecules, especially (i) the unsaturated bond between the aliphatic carbons; (ii) the ketone group; and (iii) the presence of heteroatoms. 6,11,12 The heterocyclic chalcones have a heteroaryl which contain an oxygen, sulfur or nitrogen. 12,13 The pyridine is one type of aryl group with nitrogen as heteroatom, and is assigned to numerous biological activities, such as anti-microbial, anti-tumor and anti-viral.…”

Section: Introductionmentioning

confidence: 99%

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Hirshfeld Surfaces and Nonlinear Optics on Two Conformers of a Heterocyclic Chalcone

Custódio¹,

Moreira²,

Valverde³

et al. 2017

J. Braz. Chem. Soc.

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Heterocyclic chalcones have been prominent in the scientific community due to various biological activities reported for these compounds. The structural knowledge of heterocyclic chalcones can help in the understanding of their mechanism of action. The Hirshfeld surfaces were used to study the supramolecular arrangement of two conformers present into asymmetric unit of the heterocyclic chalcone (2E)-3-(4-methylphenyl)-1-(pyridin-3-yl)-prop-2-en-1-one on crystalline state. In addition, the linear polarizability (α), the first hyperpolarizability (β||z), and the second hyperpolarizability (γ) of the conformers were calculated to get a better insight on the linear and nonlinear optical behaviors of these structures in presence of solvent medium, as well as their band-gap energies. The Hirshfeld surfaces confirmed the presence of C−H···N, C−H···O and C−H···C interactions in packaging stabilization. Finally, the 2D fingeprint plot was used to the quantification of contacts and indicated that there are both π···π and C−H···π interactions present in the compound.

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Section: Introductionmentioning

confidence: 99%

“…6,11,12 The heterocyclic chalcones have a heteroaryl which contain an oxygen, sulfur or nitrogen. 12,13 The pyridine is one type of aryl group with nitrogen as heteroatom, and is assigned to numerous biological activities, such as anti-microbial, anti-tumor and anti-viral.…”

Section: Introductionmentioning

confidence: 99%

Hirshfeld Surfaces and Nonlinear Optics on Two Conformers of a Heterocyclic Chalcone

Custódio¹,

Moreira²,

Valverde³

et al. 2017

J. Braz. Chem. Soc.

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“…In view of the literature precedent [11,12] and our above results with T. b. rhodesiense we decided to screen our compound library against Leishmania donovani [21]. Using HU3 intracellular amastigotes at 30 mM only 8, 9, 12 and 20 showed any activity, with 39.7, 13.8, 11.6 and 2.7% inhibition respectively.…”

Section: Resultsmentioning

confidence: 99%

“…Pyridylchalcones, such as 3 and 4, have been found to exhibit both antimalarial and anti-leishmanial activity [6,11,12,13]. However, there are no examples of them being tested against Trypanosoma brucei.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and antitrypanosomal activities of novel pyridylchalcones

Bhambra

Ruparelia

Tan

et al. 2017

European Journal of Medicinal Chemistry

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a b s t r a c tA library of novel pyridylchalcones were synthesised and screened against Trypanosoma brucei rhodesiense. Eight were shown to have good activity with the most potent 8 having an IC 50 value of 0.29 mM.Cytotoxicity testing with human KB cells showed a good selectivity profile for this compound with a selectivity index of 47. Little activity was seen when the library was tested against Leishmania donovani. In conclusion, pyridylchalcones are promising leads in the development of novel compounds for the treatment of human African trypanosomiasis (HAT).

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“…The conjugated double bond produces the delocalization of π electrons which reduces its electrophilic character and makes it an intermediate for the synthesis of various biologically important heterocycles such as pyrazoline, oxazoline, thiazine, oxazine, pyrimidine etc. Thus synthesis of chalcones has generated vast interest to organic as well as medicinal chemists [3]. Formation of these nuclei involves cyclization of α-β unsaturated system of chalcones.…”

Section: Introductionmentioning

confidence: 99%

Chalconoid Derived Heterocycles as Potent Bioactive Molecules: A Review

Sapra¹,

Sharma²

2016

Chem Sci J

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Although chalcones symbolize an important pharmacophore for variety of biological actions, however their analogues are also reported to be equally important for plethora of biological actions. In the present review, a comprehensive study of chalcones derived molecules (like pyrazoles, isoxazoles, pyridine, pyrimidine) their pharmacological actions, mechanism of action, structure activity relationship studies have been described. which includes anti-proliferative, anti-inflammatory, antioxidant, proapoptotic, anti-bacterial and anti-adhesive effects [18]. Analogues of chalcones Pyrazoline analogues with various pharmacological activities:Pyrazole nucleus present in compounds exhibit wide range of biological activity. Introduction of a pyrazole ring in the chalcones between the two aryl rings increase the cytotoxic activity against a series of human cancer cell lines. Dhar et al. [19] synthesized a series of 1-acetyl-3,5-diaryl-4,5-dihydro-(H)-pyrazoles and assayed for in vitro cytotoxicity against PC-3, OVCAR, IMR-32, HEP-2 human cancer cell lines, compound 1 showed broad spectrum cytotoxic activity against all the four cell lines. The activity shown by the compounds conclude that (i) Substitution on phenyl ring showed marked effect on cytotoxic activity, (ii) Presence of electron donating groups on phenyl ring led to enhanced activity whereas electron withdrawing group except NO 2 reduces the cytotoxic activity, (iii) Replacement of phenyl ring with heterocyclic ring also reduces the cytotoxic potential and napthyl ring on both sides are more beneficial for cytotoxic potential Chemical Sciences JournalChem ic a l S cience s J o u rnal

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Heteroaryl chalcones: Mini review about their therapeutic voyage

Cited by 60 publications

References 49 publications

Hirshfeld Surfaces and Nonlinear Optics on Two Conformers of a Heterocyclic Chalcone

Hirshfeld Surfaces and Nonlinear Optics on Two Conformers of a Heterocyclic Chalcone

Synthesis and antitrypanosomal activities of novel pyridylchalcones

Chalconoid Derived Heterocycles as Potent Bioactive Molecules: A Review

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