151229-84-4Relevant articles and documents
Discovery of Novel Pyrido-pyridazinone Derivatives as FER Tyrosine Kinase Inhibitors with Antitumor Activity
Taniguchi, Toru,Inagaki, Hiroaki,Baba, Daichi,Yasumatsu, Isao,Toyota, Akiko,Kaneta, Yasuyuki,Kiga, Masaki,Iimura, Shin,Odagiri, Takashi,Shibata, Yoshihiro,Ueda, Kiyono,Seo, Maki,Shimizu, Hiroki,Imaoka, Tomoki,Nakayama, Kiyoshi
supporting information, p. 737 - 742 (2019/04/01)
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.
One pot synthesis of 2,6-dichloro-3,5-dicyanopyridine from aliphatic precursors
Duindam,Lishinsky,Sikkema
, p. 2605 - 2609 (2007/10/02)
Malononitrile is condensed with triethyl orthoformate in the presence of pyridine; the mixture is acidified with HCl gas and after addition of further pyridine, HCl diazotised to form 2,6-dichloro-3,5-dicyanopyridine in a convenient, high yield process.