Synthesis and high antiproliferative activity of dehydroabietylamine pyridine derivatives in vitro and in vivo. Issue 12 (26th June 2020)

• Record Type: Journal Article
• Authors: Zhao, Fengyi; Lu, Wen; Xu, Yuanyuan; Xu, Li; Zhang, Jingjing; Sun, Xu; Yang, Shilong; Zhou, Mengyi; Su, Fan; Lin, Feng; Cao, Fuliang
• Is Part Of: Biochemical journal. Volume 477:Issue 12(2020)
• Page Start: 2383
• Page End: 2399
• Publication Date: 2020-06-26
• Subjects: amides derivatives -- antiproliferative -- apoptosis -- dehydroabietylamine schiff-base; Biochemistry -- Periodicals; 572
• DOI: 10.1042/BCJ20200337
• Languages: English
• ISSNs: 0264-6021

Abstract

Abstract : Several bioactive dehydroabietylamine Schiff-bases (L 1 −L 4 ), amides (L 5 −L 11 ) and complex CuL 3 (NO3 )2, Cu(L 5 )3, Co(L 6 )2 Cl2 had been synthesized successfully for developing more efficient but lower toxic antiproliferative compounds. Their antiproliferative activities to Hela (cervix), HepG2 (liver), MCF-7 (breast), A549 (lung) and HUVEC (umbilical vein, normal cell) were investigated in vitro . The toxicity of all compounds was less than dehydroabietylamine (L 0 ). For HepG2 cells, L 1, L 2 and L 3 had higher anti-HepG2 activity, especially L 1 (0.52 µM) had highest anti-HepG2 activity but low toxicity. For MCF-7 cells, L 1, L 2, L 3 and L 4 had higher anti-MCF-7 activity, especially L 3 (0.49 µM) had highest anti-MCF-7 activity but low toxicity. For A549 cells, L 2 and L 3 had higher anti-A549 activity. Furthermore, L 1 and L 3 may be the great promise antiproliferative drugs with nontoxic side effects, due to the high anti-HepG2 and anti-MCF-7 inhibition rate in vivo, 65% and 61%, respectively. L 1, L 2 and L 3 could induce apoptosis through intercalating into DNA.