@article{cc425432002e486bb22ef2f5e425ff22,
title = "Palladium-catalyzed N-arylation of 2-aminobenzothiazole-4-carboxylates/carboxamides: Facile synthesis of PARP14 inhibitors",
abstract = "We have developed a palladium-catalyzed N-arylation of the biologically interesting, but synthetically rather challenging 2-arylaminobenzothiazoles bearing multiple functionalities. This protocol was successfully used to readily synthesize our initial PARP14 inhibitor followed by a limited structural optimization. A more potent PARP14 inhibitor with an IC50 value of 1.69 μM was identified, and the interaction was ascertained by the X-ray co-crystal structure of the catalytic domain of PARP14 in complex with compound 8.",
keywords = "2-Arylaminobenzothiazoles, C-N coupling, N-arylation, PARP14, Pd(dba)",
author = "Pingyuan Wang and Jian Li and Xue Jiang and Zhiqing Liu and Na Ye and Youjun Xu and Guangfu Yang and Yechun Xu and Ao Zhang",
note = "Funding Information: This work was supported by grants of Chinese National Sciences Foundation ( 81125021 , 81373277 ), National Science & Technology Major Project on {\textquoteleft}Key New Drug Creation and Manufacturing Program{\textquoteright}, China (Numbers: 2012ZX09103-101-035 , 2012ZX09301001-001 ). Supporting grants from the 'Interdisciplinary Cooperation Team' Program for Science and Technology Innovation (CAS) , and grant from the State Key Laboratory of Drug Research ( SIMM1302KF-08 , SIMM1302KF-02 ), Shanghai Institute of Materia Medica were also appreciated. Publisher Copyright: {\textcopyright} 2014 Elsevier Ltd. All rights reserved. Copyright: Copyright 2020 Elsevier B.V., All rights reserved.",
year = "2014",
month = sep,
day = "2",
doi = "10.1016/j.tet.2014.06.064",
language = "English (US)",
volume = "70",
pages = "5666--5673",
journal = "Tetrahedron",
issn = "0040-4020",
publisher = "Elsevier Limited",
number = "35",
}