โ Scribed by Chih-Hung Chen; On Lee; Chung-Niang Yao; Meng-Yun Chuang; Yow-Lone Chang; May-Hua Chang; Yen-Fang Wen; Wan-Hsu Yang; Ching-Huai Ko; Nien-Tzu Chou; Mai-Wei Lin; Chin-Pen Lai; Chung-Yuan Sun; Ling-mei Wang; Yen-Chun Chen; Tzong-Hsiung Hseu; Chia-Ni Chang; Hui-Chun Hsu; Hui-Chi Lin; Yu-Li Chang; Ying-Chu Shih; Shuen-Hsiang Chou; Yi-Ling Hsu; Hsiang-Wen Tseng; Chih-Peng Liu; Chia-Mu Tu; Tsan-Lin Hu; Yuan-Jang Tsai; Ting-Shou Chen; Chih-Lung Lin; Shu-Jiau Chiou; Chung-Cheng Liu; Chrong-Shiong Hwang
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A series of azulene-based derivatives were synthesized as potent inhibitors for receptor tyrosine kinases such as FMS-like tyrosine kinase 3 (FLT-3). Systematic side chain modification of prototype 1a was carried out through SAR studies. Analogue 22 was identified from this series and found to be one of the most potent FLT-3 inhibitors, with good pharmaceutical properties, superior efficacy, and tolerability in a tumor xenograft model.
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