16349-40-9Relevant articles and documents
NOVEL HYDRAZONE DERIVATIVE WITH ARYL OR HETEROARYL GROUP SUBSTITUTED AT TERMINAL AMINE GROUP THEREOF AND USE THEREOF
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Paragraph 0362-0363; 0440-0441, (2021/11/04)
The present invention relates to novel hydrazone derivatives in which a terminal amine group is substituted with an aryl group or a heteroaryl group, and uses thereof.
Design, synthesis and antitumor activity of 6,7-disubstituted-4-(heteroarylamino)quinoline-3-carbonitrile derivatives
Liu, Bao,You, Qi Dong,Li, Zhi Yu
scheme or table, p. 554 - 557 (2011/03/17)
A series of new 6,7-disubstituted-4-(benzothiazol-6-ylamino)quinoline-3-carbonitrile derivatives (12a-l) were synthesized. The cytotoxicity of 12 new compounds was evaluated in AGS, HepG2 and HT-29 cell lines. The results showed that compounds 12g, 12h, 12i, 12k and 12l displayed more potent cytotoxic activities than Bosutinib, compound 12l exhibited the most potent antitumor activity among the tested compounds.
In vitro activities of position 2 substitution-bearing 6-nitro- and 6-amino-benzothiazoles and their corresponding anthranilic acid derivatives against Leishmania infantum and Trichomonas vaginalis.
Delmas, Florence,Di Giorgio, Carole,Robin, Maxime,Azas, Nadine,Gasquet, Monique,Detang, Claire,Costa, Muriel,Timon-David, Pierre,Galy, Jean-Pierre
, p. 2588 - 2594 (2007/10/03)
6-Nitro- and 6-amino-benzothiazoles bearing different chains in position 2 and their corresponding anthranilic acid derivatives were investigated for their in vitro antiparasitic properties against parasites of the species Leishmania infantum and Trichomonas vaginalis compared to their toxicity towards human monocytes. Biological investigations established that the antiprotozoal properties depended greatly on the chemical structure of the position 2 substitution-bearing group. Compound C1, 2-[(2-chloro-benzothiazol-6-yl) amino] benzoic acid, demonstrated an interesting antiproliferative activity towards parasites of the species T. vaginalis, while compound C11, 2-([2-[(2-hydroxyethyl) amino]-benzothiazol-6-yl] amino) benzoic acid, exhibited a promising activity against parasites of the species L. infantum in their intracellular amastigote form. Additional experiments established that compound C11, which was poorly toxic against the promastigote and the extracellular amastigote forms of the parasite, could improve host-protective mechanisms against Leishmania by preventing parasite internalization by macrophages and stimulating NO production, by means of a mechanism synergistically enhanced by the presence of gamma interferon.