Synthesis and antiproliferative activity of monocationic arylthiophene derivatives

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• 作者：Mohamed A. Ismail^a ; ^b ; ^{ismail_158@yahoo.com} ; ^{mismail@mans.edu.eg} ; Magdy M. Youssef^a ; ^b ; Reem K. Arafa^c ; Shar S. Al-Shihry^a ; Wael M. El-Sayed^d ; ^{waelelhalawany@hotmail.com} ; ^{wael_farag@sci.asu.edu.eg}
• 关键词：Monocationic arylthiophenes ; Suzuki coupling ; Antiproliferative activity ; DNA affinity ; tyrosine kinase inhibition
• 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：789-798
• 全文大小：781 K
• 卷排序：126

文摘

Presence of methoxy groups in 4b and 4c enhanced the anticancer activity. Compounds 4e and 4i with p-chlorophenyl-substitution were the most active anticancer agents with 88–98% inhibition in tyrosine kinase activity. The electron withdrawing hydrophobic substitutions are more in favor of activity than the electron donating hydrophilic ones. Novel monocationic arylthiophenes are tyrosine kinase inhibitors at nanomolar concentrations.