4.6 Article

Synthesis of New 1,3,5-Triazine-Based 2-Pyrazolines as Potential Anticancer Agents

Journal

MOLECULES
Volume 23, Issue 8, Pages -

Publisher

MDPI
DOI: 10.3390/molecules23081956

Keywords

1, 3, 5-triazines; chalcones; 2-pyrazolones; Claisen-Schmidt reaction; cyclocondensation reactions; microwave irradiation; anticancer activity

Funding

  1. Colciencias
  2. Universidad del Valle
  3. Science, Technology and Innovation Fund-General Royalties System (FCTeI-SGR) [BPIN 2013000100007]

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A new series of 1,3,5-triazine-containing 2-pyrazoline derivatives (8-11)a-g was synthesized by cyclocondensation reactions of [(4,6-bis((2-hydroxyethyl)amino)-1,3,5-triazin-2-yl)amine]chalcones 7a-g with hydrazine hydrate and derivatives. Chalcones 7a-g were obtained by Claisen-Schmidt condensation between aromatic aldehydes and triazinic derivative 5, which was synthesized in high yield by a microwave-assisted reaction. Seventeen of the synthesized compounds were selected and tested by the US National Cancer Institute (NCI) for their anticancer activity against 58 different human tumor cell lines. Compounds 7g and 10d,e,g showed important GI(50) values ranging from 0.569 to 16.6 mu M and LC50 values ranging from 5.15 to >100 mu M.

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