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

被引：49

作者：

Moreno, Leydi M. ^{[1
]}

Quiroga, Jairo ^{[1
,2
]}

Abonia, Rodrigo ^{[1
,2
]}

Ramirez-Prada, Jonathan ^{[1
]}

Insuasty, Braulio ^{[1
,2
]}

机构：

[1] Univ Valle, Dept Chem, Heterocycl Cpds Res Grp, Cali 25360, Colombia

[2] Ctr Bioinformat & Photon CIBioFI, Calle 13 100-00,Edificio 320,1069, Cali 25360, Colombia

来源：

MOLECULES | 2018年 / 23卷 / 08期

关键词：

1; 3; 5-triazines; chalcones; 2-pyrazolones; Claisen-Schmidt reaction; cyclocondensation reactions; microwave irradiation; anticancer activity; BIOLOGICAL EVALUATION; ANTIMICROBIAL ACTIVITY; ANTIMALARIAL AGENTS; MOLECULAR DOCKING; CELL-LINES; DERIVATIVES; INHIBITORS; HYBRIDS; CANCER; PYRAZOLE;

D O I：

10.3390/molecules23081956

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页数：20

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