2. Academic Validation
  3. Insights into the structure-activity relationship of the anticancer compound ZJ-101: A role played by the amide moiety

Insights into the structure-activity relationship of the anticancer compound ZJ-101: A role played by the amide moiety

  • Bioorg Med Chem Lett. 2024 Jun 1:105:129741. doi: 10.1016/j.bmcl.2024.129741.
Haibo Qiu 1,  Shan Qian 1,  Sarah A Head 2,  Phillip R Sanchez 2,  Jun O Liu 3,  Zhendong Jin 4
Affiliations

Affiliations

  • 1 Department of Pharmaceutical Sciences and Experimental Therapeutics, College of Pharmacy, The University of Iowa, Iowa City, IA 52242, USA.
  • 2 Department of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine, 725 North Wolfe St., Baltimore, MD 21205, USA.
  • 3 Department of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine, 725 North Wolfe St., Baltimore, MD 21205, USA; Department of Oncology, Johns Hopkins University School of Medicine, 725 North Wolfe St., Baltimore, MD 21205, USA.
  • 4 Department of Pharmaceutical Sciences and Experimental Therapeutics, College of Pharmacy, The University of Iowa, Iowa City, IA 52242, USA. Electronic address: zhendong-jin@uiowa.edu.
PMID: 38599296 DOI: 10.1016/j.bmcl.2024.129741
Abstract

ZJ-101, a structurally simplified analog of marine natural product superstolide A, was previously designed and synthesized in our laboratory. In the present study four new analogs of ZJ-101 were designed and synthesized to investigate the structure-activity relationship of the acetamide moiety of the molecule. The biological evaluation showed that the amide moiety is important for the molecule's Anticancer activity. Replacing the amide with Other functional groups such as a sulfonamide group, a carbamate group, and a urea group resulted in the decrease in Anticancer activity.

Keywords

Anticancer agent; SAR; Superstolide A; ZJ-101.

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  • HY-161424
    抗癌类似物
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