Several bioactive dehydroabietylamine Schiff-bases (L1−L4), amides (L5−L11) and complex CuL3(NO3)2, Cu(L5)3, Co(L6)2Cl2 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 (L0). For HepG2 cells, L1, L2 and L3 had higher anti-HepG2 activity, especially L1 (0.52 µM) had highest anti-HepG2 activity but low toxicity. For MCF-7 cells, L1, L2, L3 and L4 had higher anti-MCF-7 activity, especially L3(0.49 µM) had highest anti-MCF-7 activity but low toxicity. For A549 cells, L2 and L3 had higher anti-A549 activity. Furthermore, L1 and L3 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. L1, L2 and L3 could induce apoptosis through intercalating into DNA.
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Cover Image
The Autographa californica Multiple Nucleo-Polyhedrosis virus encodes for a variant of Ubiquitin molecule that can create atypical linkages mediated by Lysine 54 (shown in red). We show that the Ubiquitin signalling via the atypical chains is protected from the host Deubiquitinase enzymes, which possibly allows the virus to circumvent antiviral responses. For more information, see the article by Negi and colleagues in this issue (pp. 2193–2219). The image was provided by Ranabir Das.
Synthesis and high antiproliferative activity of dehydroabietylamine pyridine derivatives in vitro and in vivo
Fengyi Zhao, Wen Lu, Yuanyuan Xu, Li Xu, Jingjing Zhang, Xu Sun, Shilong Yang, Mengyi Zhou, Fan Su, Feng Lin, Fuliang Cao; Synthesis and high antiproliferative activity of dehydroabietylamine pyridine derivatives in vitro and in vivo. Biochem J 26 June 2020; 477 (12): 2383–2399. doi: https://doi.org/10.1042/BCJ20200337
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