Synthesis and in vitro cytotoxic evaluation of new quinazolinone-based conjugates

Tran Khac Vu; Nguyen Huong  Linh; Ta Hong Duc; Ho Duc Cuong

doi:10.15625/2525-2518/59/4/15624

Synthesis and in vitro cytotoxic evaluation of new quinazolinone-based conjugates

Tran Khac Vu, Nguyen Huong Linh, Ta Hong Duc, Ho Duc Cuong

Author affiliations

Authors

Tran Khac Vu School of Chemical Engineering, Hanoi University of Science and Technology, No 1, Dai Co Viet, Hai Ba Trung, Hanoi, Vietnam https://orcid.org/0000-0003-1127-1597
Nguyen Huong Linh School of Chemical Engineering, Hanoi University of Science and Technology, No 1, Dai Co Viet, Hai Ba Trung, Hanoi, Vietnam
Ta Hong Duc School of Chemical Engineering, Hanoi University of Science and Technology, No 1, Dai Co Viet, Hai Ba Trung, Hanoi, Vietnam
Ho Duc Cuong School of Chemical Engineering, Hanoi University of Science and Technology, No 1, Dai Co Viet, Hai Ba Trung, Hanoi, Vietnam

DOI:

https://doi.org/10.15625/2525-2518/59/4/15624

Keywords:

quinazolinone, cytotoxic, conjugate, cancer

Abstract

A series of new quinazolione derivatives containing a conjugate sytem 13 a-l were synthesized via a three step-procedure. The first step is the condensation of 5-hydroxyanthranilic acid (10) at 160^oC for 2 h to afford the intermediate 11 in high yield. This intermediate was then reacted with n-butylamin in acetic acid at 160^oC for 14 h to give 12 in 92%. Finally, the reaction of 12 with different aldehydes in acetic acid at 140^oC for 14h furnished new conjugates 13a-l in 62-81%. The bioassay results showed that several compounds displayed cytotoxic effect against two cell lines including HepG-2 and SKLu-1 in which 13h exhibited the strongest cytotoxic effect against SKLu-1 with IC₅₀ value of 5.05 µg/mL.

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Published

13-08-2021

How to Cite

[1]

T. K. Vu, N. H. . Linh, T. H. Duc, and H. D. Cuong, “Synthesis and in vitro cytotoxic evaluation of new quinazolinone-based conjugates ”, Vietnam J. Sci. Technol., vol. 59, no. 4, pp. 489–497, Aug. 2021.

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Vol. 59 No. 4 (2021)

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Natural Products

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