2. Academic Validation
  3. Anti-proliferative activity and structure-activity relationship of honokiol derivatives

Anti-proliferative activity and structure-activity relationship of honokiol derivatives

  • Bioorg Med Chem. 2019 Aug 15;27(16):3729-3734. doi: 10.1016/j.bmc.2019.06.042.
Ding Lin 1,  Zhongzhong Yan 2,  Aiyu Chen 2,  Jiao Ye 2,  Aixi Hu 3,  Juan Liu 4,  Junmei Peng 4,  Xiaoyun Wu 5
Affiliations

Affiliations

  • 1 College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, China; Department of Traditional Chinese Medicine, Zhejiang A & F University, Hangzhou 311300, China.
  • 2 College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, China.
  • 3 College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, China. Electronic address: axhu@hnu.edu.cnaxhu.
  • 4 College of Pharmacy and Biological Science, University of South China, Hengyang 421000, China.
  • 5 Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Science, Southern Medical University, Guangzhou 510515, China.
PMID: 31278004 DOI: 10.1016/j.bmc.2019.06.042
Abstract

As a known natural product with anti-tumor activity, honokiol has been widely researched and structural modified. Lots of honokiol derivatives have been found to possess good anti-proliferative activity and showed great potential in Cancer therapy, but the SAR (structure-activity relationship) was still confused. Here in, the SAR were comprehensively researched by summary of reported derivatives and synthesis of novel derivatives. Amongst novel derivatives, the promising compounds A6 and A10 exhibited potent and selective anti-proliferative activities against K562 cell line with the IC50 values of 5.04 and 7.08 μM respectively. The SAR was discussed around honokiol and 79 derivatives by the means of CoMFA and theoretical calculation, which provided useful suggestion for further structural optimization of honokiol derivatives.

Keywords

3D-QASR; Anti-proliferative; Honokiol; Structure-activity relationship; Theoretical calculations.

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