{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,6,8]],"date-time":"2026-06-08T18:29:51Z","timestamp":1780943391415,"version":"3.54.1"},"reference-count":28,"publisher":"Wiley","issue":"1","license":[{"start":{"date-parts":[[2023,10,18]],"date-time":"2023-10-18T00:00:00Z","timestamp":1697587200000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":["onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["Chem Biol Drug Des"],"published-print":{"date-parts":[[2024,1]]},"abstract":"<jats:title>Abstract<\/jats:title><jats:p>Ribosome S6 Protein Kinase 2 (RSK2) is involved in many signal pathways such as cell growth, proliferation, survival and migration in tumors. Also, RSK2 can phosphorylate YB\u20101, which induces the expression of tumor initiating cells, leading to poor prognosis of triple negative breast cancer. Herein, phenyl sulfonamide was introduced to a series of 1H\u2010pyrrolo[2,3\u2010b]pyridine\u20102\u2010carboxamide derivatives to obtain novel RSK2 inhibitors which were evaluated RSK2 inhibitory activity and proliferation inhibitory activity against MDA\u2010MB\u2010468. The newly introduced sulfonamide group was observed to form a hydrogen bond with target residue LEU\u201074 which played crucial role in activity. The results showed that most of compounds exhibited RSK2 enzyme inhibitory with IC<jats:sub>50<\/jats:sub> up to 1.7\u2009nM. Compound <jats:bold>B1<\/jats:bold> exhibited the strongest MDA\u2010MB\u2010468 cell anti\u2010proliferation activity (IC<jats:sub>50<\/jats:sub>\u2009=\u20090.13\u2009\u03bcM). The in\u00a0vivo tumor growth inhibitory activities were evaluated with compounds <jats:bold>B1<\/jats:bold>\u2010<jats:bold>B3<\/jats:bold> in MDA\u2010MB\u2010468 xenograft model which gave up to 54.6% of TGI.<\/jats:p>","DOI":"10.1111\/cbdd.14376","type":"journal-article","created":{"date-parts":[[2023,10,19]],"date-time":"2023-10-19T02:00:05Z","timestamp":1697680805000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":2,"title":["Synthesis and anti\u2010tumor activity evaluation of <scp>1H<\/scp>\u2010pyrrolo[2,3\u2010b]pyridine\u20102\u2010carboxamide derivatives with phenyl sulfonamide groups as potent <scp>RSK2<\/scp> inhibitors"],"prefix":"10.1111","volume":"103","author":[{"given":"Xiaoyu","family":"Zhang","sequence":"first","affiliation":[{"name":"R &amp;D Center, Nanjing Sanhome Pharmaceutical Co. Ltd. Nanjing Jiangsu China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Guochuang","family":"Zheng","sequence":"additional","affiliation":[{"name":"R &amp;D Center, Nanjing Sanhome Pharmaceutical Co. Ltd. Nanjing Jiangsu China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Shang","family":"Gao","sequence":"additional","affiliation":[{"name":"R &amp;D Center, Nanjing Sanhome Pharmaceutical Co. Ltd. Nanjing Jiangsu China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Feng","family":"Zhou","sequence":"additional","affiliation":[{"name":"R &amp;D Center, Nanjing Sanhome Pharmaceutical Co. Ltd. Nanjing Jiangsu China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Tao","family":"Pan","sequence":"additional","affiliation":[{"name":"R &amp;D Center, Nanjing Sanhome Pharmaceutical Co. Ltd. Nanjing Jiangsu China"},{"name":"School of Pharmacy China Pharmaceutical University Nanjing Jiangsu China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Qiqi","family":"Shi","sequence":"additional","affiliation":[{"name":"R &amp;D Center, Nanjing Sanhome Pharmaceutical Co. Ltd. Nanjing Jiangsu China"},{"name":"School of Pharmacy China Pharmaceutical University Nanjing Jiangsu China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jiani","family":"Li","sequence":"additional","affiliation":[{"name":"R &amp;D Center, Nanjing Sanhome Pharmaceutical Co. Ltd. Nanjing Jiangsu China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Xiaomeng","family":"Zhang","sequence":"additional","affiliation":[{"name":"R &amp;D Center, Nanjing Sanhome Pharmaceutical Co. Ltd. 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