2. Academic Validation
  3. Synthesis of the analogs of plocabulin and their preliminary structure-activity relationship study

Synthesis of the analogs of plocabulin and their preliminary structure-activity relationship study

  • Bioorg Med Chem Lett. 2021 Nov 1:51:128355. doi: 10.1016/j.bmcl.2021.128355.
Leiming Wang 1,  Xin Li 2,  Hong Cui 3,  Xinsheng Lei 3,  Hongchun Liu 4,  Quanrui Wang 5,  Yingxia Li 6
Affiliations

Affiliations

  • 1 Department of Chemistry, Fudan University, 2005 Songhu Road, Shanghai 200438, China; Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 201203, China.
  • 2 Division of Anti-tumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China.
  • 3 Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 201203, China.
  • 4 Division of Anti-tumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China. Electronic address: hchliu@simm.ac.cn.
  • 5 Department of Chemistry, Fudan University, 2005 Songhu Road, Shanghai 200438, China. Electronic address: qrwang@fudan.edu.cn.
  • 6 Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 201203, China. Electronic address: liyx417@fudan.edu.cn.
PMID: 34508844 DOI: 10.1016/j.bmcl.2021.128355
Abstract

Plocabulin, a marine natural polyketide isolated from the Sponge Lithoplocamia lithistoides, is a novel and potent microtubule-destabilizing agent. Guided by the reported binding mode, several new analogs of plocabulin have been designed through removing the right aliphatic chain and further modifying on the carbamate group and the enamide unit. The preliminary results indicate that the right aliphatic chain in plocabulin is allowed to remove with a little loss of activity, the carbamate group plays a role in the activity, and particularly, the enamide unit has an important effect on the activity. This new finding will aid the design of novel potent tubulin-binding agents based on plocabulin.

Keywords

Antiproliferation; Marine nature products; PM060184; Plocabulin; Synthesis.

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