2. Academic Validation
  3. Aromatic Ring Substituted Aaptamine Analogues as Potential Cytotoxic Agents against Extranodal Natural Killer/T-Cell Lymphoma

Aromatic Ring Substituted Aaptamine Analogues as Potential Cytotoxic Agents against Extranodal Natural Killer/T-Cell Lymphoma

  • J Nat Prod. 2020 Dec 24;83(12):3758-3763. doi: 10.1021/acs.jnatprod.0c00769.
Fan Yang 1,  Yuan Gao 1,  Yung-Ting Chang 1,  Yike Zou 2,  K N Houk 2,  Jing-Rong Lu 1,  Jing He 1,  Wei-Zhuo Tang 3,  Hong-Ze Liao 1,  Hua Han 4,  Hou-Wen Lin 1
Affiliations

Affiliations

  • 1 Research Center for Marine Drugs, State Key Laboratory of Oncogenes and Related Genes, Department of Pharmacy, Renji Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai 200127, People's Republic of China.
  • 2 Department of Chemistry and Biochemistry, University of California, Los Angeles, California 90095-1569, United States.
  • 3 College of Biological and Environmental Engineering, Changsha University, Changsha 410022, People's Republic of China.
  • 4 School of Medicine, Tongji University, Shanghai 200092, People's Republic of China.
PMID: 33170001 DOI: 10.1021/acs.jnatprod.0c00769
Abstract

A chemical modification study was conducted on the marine natural product aaptamine (1), isolated from the marine Sponge Aaptos aaptos. Thirty new derivatives substituted by various aromatic rings at the 3- and 7-positions of aaptamine were prepared by bromination, followed by the Suzuki coupling reaction. Sixteen compounds displayed cytotoxicities to four Cancer cell lines (IC50 < 10 μM). In particular, compound 5i demonstrated a significant antiproliferative effect on the extranodal natural killer/T-cell lymphoma (ENKT) cell line SNK-6 with an IC50 value of 0.6 μM. Additionally, compound 5i showed cytotoxicities to multiple lymphoma cell lines, including Ramos, Raji, WSU-DLCL2, and SU-DHL-4 cells.

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