Synthesis and Biological Evaluation of PF-543 Derivative Containing Aliphatic Side Chain
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- Kim Seon Woong
- College of Pharmacy and Natural Medicine Research Institute, Mokpo National University
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- Lee Taeho
- College of Pharmacy, Research Institute of Pharmaceutical Sciences, Kyungpook National University
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- Oh Yoon Sin
- Department of Food and Nutrition, Eulji University
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- Shin Sang Mi
- College of Pharmacy, Chosun University
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- Lee Joo-Youn
- College of Pharmacy, Seoul National University Korea Chemical Bank, Korea Research Institute of Chemical Technology
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- Kim Sanghee
- College of Pharmacy, Seoul National University
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- Baek Dong Jae
- College of Pharmacy and Natural Medicine Research Institute, Mokpo National University
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- Park Eun-Young
- College of Pharmacy and Natural Medicine Research Institute, Mokpo National University
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<p>The PF-543 is known as a potent and selective inhibitor of sphingosine kinase (SK) 1 amongst all the SK inhibitors known to date. In a recently reported study by Pfizer on the synthesis of PF-543 derivatives and the SK inhibitory effects, the introduction of propyl moiety into sulfonyl group of PF-543 in the case of 26b revealed an excellent result of 1.7 nM of IC50 of SK1, suggesting the potential substitution of chain structure for benzenesulfonyl structure. In the present work, we aimed for identification of antitumor activity and inhibitory effects of PF-543 derivative containing aliphatic long chain (similar to known SK inhibitors) on SK1. The synthesized compound 2 exhibited an inhibitory effect on SK1 in a manner similar to that of PF-543; the PF-543 derivative manifested similar antitumor activity on HT29, HCT116 (colorectal cancer cell line), and AGS (gastric cancer cell line) cells. Also, from the docking study conducted with PF-543 and compound 2, it was apparent that the aliphatic chain in compound 2 could probably replace benzenesulfonyl structure of PF-543.</p>
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 67 (6), 599-603, 2019-06-01
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390282763118826752
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- NII論文ID
- 130007657410
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- NII書誌ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 029698590
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- PubMed
- 31155566
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
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- PubMed
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