2. Academic Validation
  3. Design, synthesis, and study of novel phenethyl-based antitumor phospholipids downregulating p38 mitogen-activated protein kinase

Design, synthesis, and study of novel phenethyl-based antitumor phospholipids downregulating p38 mitogen-activated protein kinase

  • J Enzyme Inhib Med Chem. 2023 Dec;38(1):2217695. doi: 10.1080/14756366.2023.2217695.
Ahmed H E Hassan 1 2,  Yeon Il Oh 3,  Chae Hyeon Lee 4,  Yeon Ju Kim 4,  Soo Bin Cho 4,  Md Maqusood Alam 3,  Sang-Eun Park 5 6,  Kyung-Sook Chung 5,  Kyung-Tae Lee 5 6,  Yong Sup Lee 2 3 4
Affiliations

Affiliations

  • 1 Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt.
  • 2 Medicinal Chemistry Laboratory, Department of Pharmacy, College of Pharmacy, Kyung Hee University, Seoul, Republic of Korea.
  • 3 Department of Life and Nanopharmaceutical Sciences, Kyung Hee University, Seoul, Republic of Korea.
  • 4 Department of Fundamental Pharmaceutical Sciences, Kyung Hee University, Seoul, Republic of Korea.
  • 5 Department of Pharmaceutical Biochemistry, College of Pharmacy, Kyung Hee University, Seoul, Republic of Korea.
  • 6 Department of Life and Biomedical and Pharmaceutical Sciences, College of Pharmacy, Kyung Hee University, Seoul, Republic of Korea.
PMID: 37246947 DOI: 10.1080/14756366.2023.2217695
Abstract

Phenethyl-based edelfosine-analogs with saturated, monounsaturated, or polyunsaturated alkoxy substituents on phenyl ring were designed as novel antitumor lipids modulating p38 MAPK. Evaluation of the synthesised compounds against nine panels of diverse Cancer cells presented saturated and monounsaturated alkoxy-substituted derivatives as the most active than other derivatives. In addition, ortho-substituted compounds were more active than meta- or ortho-substituted compounds. They were potential Anticancer agents against blood, lung, colon, CNS, ovary, renal, and prostate cancers but not against skin nor breast cancers. Compounds, 1b and 1a emerged as the most potential Anticancer agents. Assessment of compound 1b impact on p38 MAPK and Akt confirmed it as an inhibitor of p38 MAPK but not Akt. In silico study suggested compounds 1b and 1a as possible binders to the lipid binding pocket of p38 MAPK. Overall, compounds 1b and 1a as novel broad spectrum antitumor lipids modulating activity of p38 MAPK for further development.

Keywords

Antitumor lipids; Cancer; Phospholipids; p38 MAPK.

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