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 160oC for 2 h to afford the intermediate 11 in high yield. This intermediate was then reacted with n-butylamin in acetic acid at 160oC for 14 h to give 12 in 92%. Finally, the reaction of 12 with different aldehydes in acetic acid at 140oC 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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Section

Natural Products