2. Academic Validation
  3. Synthesis and potential antineoplastic activity of dehydroabietylamine imidazole derivatives

Synthesis and potential antineoplastic activity of dehydroabietylamine imidazole derivatives

  • Medchemcomm. 2018 Nov 12;9(12):2091-2099. doi: 10.1039/c8md00487k.
Fengyi Zhao 1 2,  Wen Lu 2,  Fan Su 3,  Li Xu 2 4 5,  Dong Jiang 2,  Xu Sun 3 6,  Jiuzhou Shi 2,  Mengyi Zhou 3,  Feng Lin 3,  Fuliang Cao 1 4
Affiliations

Affiliations

  • 1 College of Forestry , Nanjing Forestry University , Nanjing 210037 , PR China . Email: xuliqby@njfu.edu.cn.
  • 2 College of Science , Nanjing Forestry University , Nanjing 210037 , PR China.
  • 3 Advanced Analysis and Testing Centre , Nanjing Forestry University , Nanjing 210037 , PR China.
  • 4 Co-Innovation Centre for Sustainable Forestry in Southern China , Nanjing Forestry University , China.
  • 5 Sate Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources , Guangxi Normal University , Guilin 541001 , PR China.
  • 6 College of Information Science and Technology , Nanjing Forestry University , Nanjing 210037 , PR China.
PMID: 30746067 DOI: 10.1039/c8md00487k
Abstract

To seek more efficient and lower toxicity Anticancer compounds, several imidazole combining dehydroabietylamine derivatives including organic salts (L 1 -L 2 ) and amides (L 3 -L 5 ) were synthesized. Their antineoplastic activity against HeLa (cervix), MCF-7 (breast), A549 (lung) and HepG2 (liver) cells and HUVECs (umbilical vein, normal cells) in vitro were evaluated by MTT assay. The results unequivocally showed that nearly all compounds had better antineoplastic activity and lower toxicity than dehydroabietylamine (L 0 ). For MCF-7 cells, L 2 (0.75 μM) and L 5 (2.17 μM) had higher anti-MCF-7 activity than L 0 and DOX. For A549 cells, L 1 (1.85 μM) and L 2 (4.37 μM) had higher anti-A549 activity than L 0 ; in particular, the IC50 value of L 1 was much lower than that of DOX. Among these investigated compounds, L 2 and L 5 had lower IC50 values (0.75 μM and 2.17 μM) against MCF-7 cells and lower toxicity, which suggested that they may be potential future Anticancer drugs. In addition, L 1 and L 2 could suppress Cancer cell proliferation by inducing Apoptosis. L 1 -L 5 could bind with DNA through intercalation.

Figures