1,2,3-Triazolyl ester of Ketorolac: A “Click Chemistry”-based highly potent PAK1-blocking cancer-killer

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• 作者：Binh Cao Quan Nguyen^a ; ^c ; ¹ ; Hideaki Takahashi^b ; ¹ ; Yoshihiro Uto^b ; ; M.d. Shahinozzaman^a ; ^c ; Shinkichi Tawata^a ; Hiroshi Maruta^a ; ^d ; ^{maruta20420@yahoo.co.jp}
• 关键词：PAK1 ; COX-2 ; Ketorolac ; Click chemistry ; Triazole ring ; Cancer
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：270-276
• 全文大小：704 K
• 卷排序：126

文摘

“Click-Chemistry”-based esterization at the COOH of “Ketorolac” boosts the anti-cancer activity by over 500-fold. The anti-cancer activity was boosted in parallel with the anti-PAK1 activity. This outcome is seemingly due to a robust increase in its cell-permeability.