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Synlett
DOI: 10.1055/a-2595-7004
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Synthesis of a 5,6-Dihydropyran-2-one Derivative with Dual Anti-Cell Migration and Anticancer Activity

Ahmed K. Hamdy
1   Medicinal and Biological Chemistry Science Farm Joint Research Laboratory, Faculty of Life Sciences, Kumamoto University, Kumamoto, Japan (Ringgold ID: RIN13205)
2   Collaborative Research Program with the Chemo-Sero-Therapeutic Research Institute for Anti-viral Agents and Hematological Diseases, Joint Research Center for Human Retrovirus Infection, Kumamoto University, Kumamoto, Japan (Ringgold ID: RIN13205)
3   Department of Medicinal Chemistry, Assiut University, Asyut, Egypt (Ringgold ID: RIN68796)
,
Hiroshi Araki
4   Research & Development, Link Genomics Ltd, Tokyo, Japan
,
Hiroshi Tateishi
1   Medicinal and Biological Chemistry Science Farm Joint Research Laboratory, Faculty of Life Sciences, Kumamoto University, Kumamoto, Japan (Ringgold ID: RIN13205)
,
Tsugumasa Toma
1   Medicinal and Biological Chemistry Science Farm Joint Research Laboratory, Faculty of Life Sciences, Kumamoto University, Kumamoto, Japan (Ringgold ID: RIN13205)
,
Mohamed O. Radwan
1   Medicinal and Biological Chemistry Science Farm Joint Research Laboratory, Faculty of Life Sciences, Kumamoto University, Kumamoto, Japan (Ringgold ID: RIN13205)
,
Shashwata Biswas
2   Collaborative Research Program with the Chemo-Sero-Therapeutic Research Institute for Anti-viral Agents and Hematological Diseases, Joint Research Center for Human Retrovirus Infection, Kumamoto University, Kumamoto, Japan (Ringgold ID: RIN13205)
,
Takeo Kuwata
2   Collaborative Research Program with the Chemo-Sero-Therapeutic Research Institute for Anti-viral Agents and Hematological Diseases, Joint Research Center for Human Retrovirus Infection, Kumamoto University, Kumamoto, Japan (Ringgold ID: RIN13205)
,
Shuzo Matsushita
2   Collaborative Research Program with the Chemo-Sero-Therapeutic Research Institute for Anti-viral Agents and Hematological Diseases, Joint Research Center for Human Retrovirus Infection, Kumamoto University, Kumamoto, Japan (Ringgold ID: RIN13205)
,
Mikako Fujita
1   Medicinal and Biological Chemistry Science Farm Joint Research Laboratory, Faculty of Life Sciences, Kumamoto University, Kumamoto, Japan (Ringgold ID: RIN13205)
,
Shin-ichiro Niwa
4   Research & Development, Link Genomics Ltd, Tokyo, Japan
,
Masami Otsuka
5   Faculty of Life Sciences, Kumamoto University, Kumamoto City, Japan
› Author AffiliationsSupported by: Japan Society for the Promotion of Science 17H03999
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5,6-Dihdropyran-2-one scaffold is found in several biological compounds. In this study, we synthesized its new derivative named PY801. This compound (1 μM) was shown to suppress migration of lung cancer cells. Furthermore, as results of cancer cell line panel experiments, PY801 showed cytotoxicity against specific cell lines. IC50 of PY801 against colorectal cancer cells HCT116 and breast cancer cells MCF7 were determined to be 8.9 and 9.3 μM, respectively, and the values are lower than those of an anticancer drug cisplatin. Compared with IC50 against peripheral blood mononuclear cells (PBMC) from a healthy donor, the selectivity index was determined to be >7. This study shows PY801 would be a new lead for anti-cell migration and anticancer drugs.



Publication History

Received: 27 February 2025

Accepted after revision: 28 April 2025

Accepted Manuscript online:
28 April 2025

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