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Prediction of Antitumor Activity of 3-substituted Quinazolinone Derivatives Synthesized in One-pot Method Catalyzed by Bi(Otf)3


Affiliations
1 Department of Medicinal Chemistry, National University of Pharmacy, Pushkinska 53, 61002, Kharkiv,, Ukraine
2 Department of Chemistry, Vikrama Simhapuri University, Nellore-524001, Andhra Pradesh,, India
     

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A series of 3-substituted guinazolinone derivatives have been synthesized in good to excellent yields and high selectivity by one-pot reaction using anthranilic acid, amine and orthoester in ethanol under mild conditions, respectively. The reaction was efficiently promoted by Bi(OTf)3 and the catalyst could be recovered easily after the reactions and reused without evident loss of reactivity. Docking studies have shown that the tested molecules have an affinity for anticancer targets. The data obtained can be used in planning experimental screening for antitumor activity.

Keywords

Synthesis, Bi(OTf)3, anthranilic acid, orthoester, one-pot union, аmine, quinazolinone derivatives, molecular docking, antitumor activity.
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  • Prediction of Antitumor Activity of 3-substituted Quinazolinone Derivatives Synthesized in One-pot Method Catalyzed by Bi(Otf)3

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Authors

L. Perekhoda
Department of Medicinal Chemistry, National University of Pharmacy, Pushkinska 53, 61002, Kharkiv,, Ukraine
M. Hari Krishna
Department of Chemistry, Vikrama Simhapuri University, Nellore-524001, Andhra Pradesh,, India
T . Sekhar
Department of Chemistry, Vikrama Simhapuri University, Nellore-524001, Andhra Pradesh,, India
A. Venkateswarlu
Department of Chemistry, Vikrama Simhapuri University, Nellore-524001, Andhra Pradesh,, India
P. Thriveni
Department of Chemistry, Vikrama Simhapuri University, Nellore-524001, Andhra Pradesh,, India
M. Suleiman
Department of Medicinal Chemistry, National University of Pharmacy, Pushkinska 53, 61002, Kharkiv,, Ukraine
A. Semenets
Department of Medicinal Chemistry, National University of Pharmacy, Pushkinska 53, 61002, Kharkiv,, Ukraine
A. Fedosov
Department of Medicinal Chemistry, National University of Pharmacy, Pushkinska 53, 61002, Kharkiv,, Ukraine
L. Grinevich
Department of Medicinal Chemistry, National University of Pharmacy, Pushkinska 53, 61002, Kharkiv,, Ukraine
N. Kobzar
Department of Medicinal Chemistry, National University of Pharmacy, Pushkinska 53, 61002, Kharkiv,, Ukraine
V. Yaremenko
Department of Medicinal Chemistry, National University of Pharmacy, Pushkinska 53, 61002, Kharkiv,, Ukraine

Abstract


A series of 3-substituted guinazolinone derivatives have been synthesized in good to excellent yields and high selectivity by one-pot reaction using anthranilic acid, amine and orthoester in ethanol under mild conditions, respectively. The reaction was efficiently promoted by Bi(OTf)3 and the catalyst could be recovered easily after the reactions and reused without evident loss of reactivity. Docking studies have shown that the tested molecules have an affinity for anticancer targets. The data obtained can be used in planning experimental screening for antitumor activity.

Keywords


Synthesis, Bi(OTf)3, anthranilic acid, orthoester, one-pot union, аmine, quinazolinone derivatives, molecular docking, antitumor activity.

References