Small-molecule inhibition of STAT3 in radioresistant head and neck squamous cell carcinoma

• Published in: Oncotarget Vol. 7; no. 18; pp. 26307 - 26330
• Main Authors: Bharadwaj, Uddalak, Eckols, T. Kris, Xu, Xuejun, Kasembeli, Moses M., Chen, Yunyun, Adachi, Makoto, Song, Yongcheng, Mo, Qianxing, Lai, Stephen Y., Tweardy, David J.
• Format: Journal Article
• Language: English
• Published: United States Impact Journals LLC 03.05.2016
• Subjects: Animals; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - pharmacology; Carcinoma, Squamous Cell - drug therapy; Cell Line, Tumor; Cell Proliferation - drug effects; Drug Screening Assays, Antitumor; Head and Neck Neoplasms - drug therapy; Humans; Mice; Mice, Nude; Naphthols - chemical synthesis; Naphthols - pharmacology; Radiation Tolerance - drug effects; Research Paper; Squamous Cell Carcinoma of Head and Neck; STAT3 Transcription Factor - antagonists & inhibitors; Sulfonamides - chemical synthesis; Sulfonamides - pharmacology; Xenograft Model Antitumor Assays; small molecule; cancer; C188-9; HNSCC; STAT3

While STAT3 has been validated as a target for treatment of many cancers, including head and neck squamous cell carcinoma (HNSCC), a STAT3 inhibitor is yet to enter the clinic. We used the scaffold of C188, a small-molecule STAT3 inhibitor previously identified by us, in a hit-to-lead program to ide...