Volume 17, Issue 17 e202200450
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Front Cover: Development of Fluorophosphoramidate as a Biocompatibly Transformable Functional Group and its Application as a Phosphate Prodrug for Nucleoside Analogs (ChemMedChem 17/2022)

Yuki Yoshida

Yuki Yoshida

Graduate School of Science, Department of Chemistry, Nagoya University, Furo-cho, Chikusa-ku, Nagoya, Aichi, 464-8602 Japan

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Ti Zheng

Ti Zheng

Graduate School of Science, Department of Chemistry, Nagoya University, Furo-cho, Chikusa-ku, Nagoya, Aichi, 464-8602 Japan

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Wataru Tanabe

Wataru Tanabe

Graduate School of Science, Department of Chemistry, Nagoya University, Furo-cho, Chikusa-ku, Nagoya, Aichi, 464-8602 Japan

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Dr. Fumiaki Tomoike

Dr. Fumiaki Tomoike

Research Center for Material Science, Nagoya University, Furo-cho, Chikusa-ku, Nagoya, Aichi, 464-8602 Japan

Department of Life Science, Gakushuin University, 15-1 Mejiro, Toshima-ku, Tokyo, 171-8588 Japan

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Dr. Fumitaka Hashiya

Dr. Fumitaka Hashiya

Research Center for Material Science, Nagoya University, Furo-cho, Chikusa-ku, Nagoya, Aichi, 464-8602 Japan

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Prof. Dr. Tetsuro Suzuki

Prof. Dr. Tetsuro Suzuki

Department of Virology and Parasitology, Hamamatsu University School of Medicine, 1-20-1 Handayama, Higashi-ku, Hamamatsu, Shizuoka, 431-3192 Japan

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Shuto Hirota

Shuto Hirota

Department of Molecular Pathology, School of Medicine, Tohoku University, Seiryo-machi, Aoba-ku, Sendai, Miyagi, 980-8575 Japan

Department of Investigative Pathology, School of Medicine, Tohoku University, Seiryo-machi, Aoba-ku, Sendai, Miyagi, 980-8575 Japan

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Dr. Yuriko Saiki

Dr. Yuriko Saiki

Department of Molecular Pathology, School of Medicine, Tohoku University, Seiryo-machi, Aoba-ku, Sendai, Miyagi, 980-8575 Japan

Department of Investigative Pathology, School of Medicine, Tohoku University, Seiryo-machi, Aoba-ku, Sendai, Miyagi, 980-8575 Japan

Office of Medical Education, School of Medicine, Tohoku University, Seiryo-machi, Aoba-ku, Sendai, Miyagi, 980-8575 Japan

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Prof. Dr. Akira Horii

Prof. Dr. Akira Horii

Department of Molecular Pathology, School of Medicine, Tohoku University, Seiryo-machi, Aoba-ku, Sendai, Miyagi, 980-8575 Japan

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Dr. Akiyoshi Hirayama

Dr. Akiyoshi Hirayama

Institute for Advanced Biosciences, Keio University, Kakuganji 246-2, Mizukami, Tsuruoka, Yamagata, 997-0052 Japan

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Prof. Dr. Tomoyosi Soga

Prof. Dr. Tomoyosi Soga

Institute for Advanced Biosciences, Keio University, Kakuganji 246-2, Mizukami, Tsuruoka, Yamagata, 997-0052 Japan

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Dr. Yasuaki Kimura

Dr. Yasuaki Kimura

Graduate School of Science, Department of Chemistry, Nagoya University, Furo-cho, Chikusa-ku, Nagoya, Aichi, 464-8602 Japan

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Prof. Dr. Hiroshi Abe

Corresponding Author

Prof. Dr. Hiroshi Abe

Graduate School of Science, Department of Chemistry, Nagoya University, Furo-cho, Chikusa-ku, Nagoya, Aichi, 464-8602 Japan

CREST, Japan Science and Technology Agency 7, Gobancho, Chiyoda-ku, Tokyo, 102-0076 Japan

Institute for Glyco-core Research (iGCORE), Tokai National Higher Education and Research System, Furo-cho, Chikusa-ku, Nagoya, Aichi, 464-8601 Japan

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First published: 07 September 2022

Graphical Abstract

The Front Cover shows a new type of biocompatible phosphate analog, a fluorophosphoramidate (FPA) functional group with characteristic P–F and P–N bonds. The stability of the FPA group was found to vary depending on the number of the amino group substitutions. Taking advantage of this intriguing molecular profile, gemcitabine FPA-prodrug, which was designed to be efficiently converted to the corresponding monophosphate in cells, showed superior anticancer activity compared with the parent compound gemcitabine and its ProTide prodrug. More information can be found in the Research Article by Yuki Yoshida, Hiroshi Abe et al.