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Efficient synthesis of 3-O-thia-cPA and preliminary analysis of its biological activity toward autotaxin |
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| Authors: | Tanaka Ryo Kato Masaru Suzuki Takahiro Nakazaki Atsuo Nozaki Emi Gotoh Mari Murakami-Murofushi Kimiko Kobayashi Susumu |
| Affiliation: | a Faculty of Pharmaceutical Sciences, Tokyo University of Science (RIKADAI), 2641 Yamazaki, Noda-shi, Chiba 278-8510, Japan b Department of Biology, Faculty of Science, Ochanomizu University, 2-1-1 Ohtsuka, Bunkyo-ku 112-8610, Tokyo, Japan |
| Abstract: | The efficient synthesis of 3-O-thia-cPAs (4a-d), sulfur analogues of cyclic phosphatidic acid (cPA), has been achieved. The key step of the synthesis is an intramolecular Arbuzov reaction to construct the cyclic thiophosphate moiety. The present synthetic route enables the synthesis of 4a-d in only four steps from the commercially available glycidol. Preliminary biological experiments showed that 4a-d exhibited a similar inhibitory effect on autotaxin (ATX) as original cPA. |
| Keywords: | Cyclic phosphatidic acid 3-O-thia-cPA Autotaxin Intramolecular Arbuzov reaction |
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