-transparent.png){kind=logo}
Discovery of Novel Pyrido-pyridazinone Derivatives as FER Tyrosine Kinase Inhibitors with Antitumor Activity. 2019
Toru Taniguchi, and
Hiroaki Inagaki, and
Daichi Baba, and
Isao Yasumatsu, and
Akiko Toyota, and
Yasuyuki Kaneta, and
Masaki Kiga, and
Shin Iimura, and
Takashi Odagiri, and
Yoshihiro Shibata, and
Kiyono Ueda, and
Maki Seo, and
Hiroki Shimizu, and
Tomoki Imaoka, and
Kiyoshi Nakayama
R&D Division, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
To obtain a new anticancer drug, we focused on FER tyrosine kinase. Starting with high-throughput screening with our in-house chemical library, compound 1, which has a pyridine moiety, was found. Referring to their X-ray crystal structure with FES proto-oncogene tyrosine kinase, as a surrogate of FER followed by chemical modification including scaffold hopping of the pyridine template, we discovered pyrido-pyridazinone derivatives with potent FER kinase inhibitory activity. Here, we disclose the structure-activity relationship on the scaffold and representative compound 21 (DS21360717), which showed in vivo antitumor efficacy in a subcutaneous tumor model.
| UI | MeSH Term | Description | Entries |
|---|
Related Publications
Toru Taniguchi, and
Hiroaki Inagaki, and
Daichi Baba, and
Isao Yasumatsu, and
Akiko Toyota, and
Yasuyuki Kaneta, and
Masaki Kiga, and
Shin Iimura, and
Takashi Odagiri, and
Yoshihiro Shibata, and
Kiyono Ueda, and
Maki Seo, and
Hiroki Shimizu, and
Tomoki Imaoka, and
Kiyoshi Nakayama
April 2016,
Archives of pharmacal research,
Toru Taniguchi, and
Hiroaki Inagaki, and
Daichi Baba, and
Isao Yasumatsu, and
Akiko Toyota, and
Yasuyuki Kaneta, and
Masaki Kiga, and
Shin Iimura, and
Takashi Odagiri, and
Yoshihiro Shibata, and
Kiyono Ueda, and
Maki Seo, and
Hiroki Shimizu, and
Tomoki Imaoka, and
Kiyoshi Nakayama
May 2013,
European journal of medicinal chemistry,
Toru Taniguchi, and
Hiroaki Inagaki, and
Daichi Baba, and
Isao Yasumatsu, and
Akiko Toyota, and
Yasuyuki Kaneta, and
Masaki Kiga, and
Shin Iimura, and
Takashi Odagiri, and
Yoshihiro Shibata, and
Kiyono Ueda, and
Maki Seo, and
Hiroki Shimizu, and
Tomoki Imaoka, and
Kiyoshi Nakayama
February 2022,
Bioorganic chemistry,
Toru Taniguchi, and
Hiroaki Inagaki, and
Daichi Baba, and
Isao Yasumatsu, and
Akiko Toyota, and
Yasuyuki Kaneta, and
Masaki Kiga, and
Shin Iimura, and
Takashi Odagiri, and
Yoshihiro Shibata, and
Kiyono Ueda, and
Maki Seo, and
Hiroki Shimizu, and
Tomoki Imaoka, and
Kiyoshi Nakayama
December 2017,
European journal of medicinal chemistry,
Toru Taniguchi, and
Hiroaki Inagaki, and
Daichi Baba, and
Isao Yasumatsu, and
Akiko Toyota, and
Yasuyuki Kaneta, and
Masaki Kiga, and
Shin Iimura, and
Takashi Odagiri, and
Yoshihiro Shibata, and
Kiyono Ueda, and
Maki Seo, and
Hiroki Shimizu, and
Tomoki Imaoka, and
Kiyoshi Nakayama
November 2019,
Bioorganic chemistry,
Toru Taniguchi, and
Hiroaki Inagaki, and
Daichi Baba, and
Isao Yasumatsu, and
Akiko Toyota, and
Yasuyuki Kaneta, and
Masaki Kiga, and
Shin Iimura, and
Takashi Odagiri, and
Yoshihiro Shibata, and
Kiyono Ueda, and
Maki Seo, and
Hiroki Shimizu, and
Tomoki Imaoka, and
Kiyoshi Nakayama
May 2023,
Bioorganic & medicinal chemistry,
Toru Taniguchi, and
Hiroaki Inagaki, and
Daichi Baba, and
Isao Yasumatsu, and
Akiko Toyota, and
Yasuyuki Kaneta, and
Masaki Kiga, and
Shin Iimura, and
Takashi Odagiri, and
Yoshihiro Shibata, and
Kiyono Ueda, and
Maki Seo, and
Hiroki Shimizu, and
Tomoki Imaoka, and
Kiyoshi Nakayama
April 2024,
European journal of medicinal chemistry,
Toru Taniguchi, and
Hiroaki Inagaki, and
Daichi Baba, and
Isao Yasumatsu, and
Akiko Toyota, and
Yasuyuki Kaneta, and
Masaki Kiga, and
Shin Iimura, and
Takashi Odagiri, and
Yoshihiro Shibata, and
Kiyono Ueda, and
Maki Seo, and
Hiroki Shimizu, and
Tomoki Imaoka, and
Kiyoshi Nakayama
March 2019,
Bioorganic & medicinal chemistry,
Toru Taniguchi, and
Hiroaki Inagaki, and
Daichi Baba, and
Isao Yasumatsu, and
Akiko Toyota, and
Yasuyuki Kaneta, and
Masaki Kiga, and
Shin Iimura, and
Takashi Odagiri, and
Yoshihiro Shibata, and
Kiyono Ueda, and
Maki Seo, and
Hiroki Shimizu, and
Tomoki Imaoka, and
Kiyoshi Nakayama
October 2020,
International journal of molecular sciences,
Toru Taniguchi, and
Hiroaki Inagaki, and
Daichi Baba, and
Isao Yasumatsu, and
Akiko Toyota, and
Yasuyuki Kaneta, and
Masaki Kiga, and
Shin Iimura, and
Takashi Odagiri, and
Yoshihiro Shibata, and
Kiyono Ueda, and
Maki Seo, and
Hiroki Shimizu, and
Tomoki Imaoka, and
Kiyoshi Nakayama
August 1994,
Anti-cancer drug design,
