Synthesis of Isoxazoles and Quinoxalines as Potential Anticancer Agents.

Vekariya, Nikhil; Khunt, M. D.; Parikh, Arun

doi:10.1002/chin.200322165

Cited by 3 publications

(4 citation statements)

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“…Compounds (63,64) bearing hydroxyl group at meta or para position of 2-and 6-phenyl rings in combination with 2-furyl, 2-thienyl, or 3-thienyl moiety at 4-position of central pyridine showed significant topo II inhibitory activity and cytotoxicity [84]. In addition, trihydroxylated derivatives are more potent topoisomerase II inhibitors and cytotoxic agents in comparison to dihydroxylated derivatives and similar author also reported topoisomerase II inhibition and cytotoxic potential of monohydroxylated pyridine derivatives (64,65). Amongst all trihydroxy derivates of pyridine proved to be the most potent agents against topoisomerase II and cytotoxicity [85,86].…”

Section: Analogues Of Chalcones Pyrazoline Analogues With Various Phamentioning

confidence: 67%

“…Solankee et al reported the synthesis of series of substituted isoxazolines and these were screened for antimicrobial activity against gram-positive, gram-negative bacteria and fungal strains, compound 53 has shown good activity against all the strains which states that compound having methoxy, chloro and nitro groups are more potent as compared to others [64]. Benzimidazole isoxazole were synthesized and screened for antimicrobial and anticancer activity and compound 54 has shown 18-25 mm zone of inhibition against antimicrobial strains and isoxazole moiety bearing molecule showed better anticancer activity [65]. Combrestatin analogues having five membered heterocycles (isoxazole, isoxazoline, oxadiazole) were synthesized and evaluated for cytotoxicity and their ability to inhibit the tubulin assembly.…”

Section: Analogues Of Chalcones Pyrazoline Analogues With Various Phamentioning

confidence: 99%

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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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Section: Analogues Of Chalcones Pyrazoline Analogues With Various Phamentioning

confidence: 67%

Section: Analogues Of Chalcones Pyrazoline Analogues With Various Phamentioning

confidence: 99%

Chalconoid Derived Heterocycles as Potent Bioactive Molecules: A Review

Sapra¹,

Sharma²

2016

Chem Sci J

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“…The reaction of chalcones with hydroxylamine hydrochloride can also be performed in the presence of NaOAc and glacial acetic acid to give 3,5diarylisoxazoles [92,93]. Using the same conditions, the condensation of benzimidazolyl-, benzofuranyl-, indolyl-and quinoxalinyltype chalcones with hydroxylamine hydrochloride provided, respectively, benzimidazolyl- [94], benzofuranyl- [95], indolyl- [96] and quinoxalinyl-isoxazoles [97].…”

Section: Transformation Of Chalcones To Isoxazolesmentioning

confidence: 99%

Chalcones as Versatile Synthons for the Synthesis of 5- and 6-membered Nitrogen Heterocycles

Albuquerque¹,

Santos²,

Cavaleiro³

et al. 2014

COC

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Chalcones belong to the flavonoid family which constitutes one of the major classes of naturally occurring oxygen heterocyclic compounds. The ,-unsaturated carbonyl system of chalcones possesses two electrophilic reactive centers allowing them to participate in addition reactions via attack to the carbonyl group (1,2-addition) or involving the-carbon (1,4-conjugate addition), leading to the synthesis of promising bioactive heterocyclic compounds. The purpose of this review is to present a systematic survey of the most recent literature that uses chalcones in the synthesis of biologically active 5-and 6-membered nitrogen heterocycles such as pyrroles, indoles, isoxazoles, imidazoles, pyrazoles, indazoles, triazoles, tetrazoles, pyridines and pyrimidines. Efficiency, easy-to-handle and cheap reagents, alternative heating conditions and greener protocols will be highlighted. In this review we will cover the literature since the beginning of the 21 st century in more than 400 publications.

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“…H 2 SO 4 (2 drops) for 30 minutes. The product obtained was filtered, dried and recrystallized from ethanol 21 Metal estimation: Metal estimation for Cu(II), Co(III) and Fe(III) complexes was done by incineration method. The metal complexes were taken in a silica crucible.…”

Section: Synthesis Of 2-benzoyl-3-nitrophenyl Quinoxalinementioning

confidence: 99%

Untitled

2014

IJPSR

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A new series of transition metal complexes of the type ML where M = Cu(II), Co(III) and Fe(III) and L = 2-benzoyl-3-(nitrophenyl)quinoxaline have been characterized and the structural features were arrived from the elemental analysis, magnetic susceptibility, molar conductance, FT-IR, UV-Vis and NMR spectral data. From the spectral measurements and magnetic susceptibility values a square planar geometry was proposed for Cu(II) complex and an octahedral geometry for Co(III) and Fe(III) complexes. The qualitative and quantitative antimicrobial activity test results proved that all the prepared complexes are very active especially against E. coli, S. aureus, C. albicans and A. niger.

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Synthesis of Isoxazoles and Quinoxalines as Potential Anticancer Agents.

Cited by 3 publications

References 0 publications

Chalconoid Derived Heterocycles as Potent Bioactive Molecules: A Review

Chalconoid Derived Heterocycles as Potent Bioactive Molecules: A Review

Chalcones as Versatile Synthons for the Synthesis of 5- and 6-membered Nitrogen Heterocycles

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