Identification of new pyrrolo[2,3-d]pyrimidines as Src tyrosine kinase inhibitors in vitro active against Glioblastoma

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• 作者：Francesca Musumeci^a ; ¹ ; Anna Lucia Fallacara^b ; ¹ ; Chiara Brullo^a ; Giancarlo Grossi^a ; Lorenzo Botta^c ; Pierpaolo Calandro^b ; Mario Chiariello^d ; Miroslava Kissova^e ; Emmanuele Crespan^e ; Giovanni Maga^e ; Silvia Schenone^a ; ^{schensil@unige.it}
• 关键词：Pyrrolo-pyrimidines ; Src ; Glioblastoma ; Kinase inhibitors ; Small molecules
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：127
• 期：Complete
• 页码：369-378
• 全文大小：1386 K
• 卷排序：127

文摘

The synthesis of 10 new pyrrolo[3,4-d]pyrimidines derivatives is reported. Molecular modeling studies showed pyrrolo-pyrimidine derivatives can efficiently bind the ATP-binding site of c-Src kinase. The synthesized compounds have been tested on a small panel of kinases. One hit compound demonstrated a very interesting cytotoxic effect against U87 Glioblastoma cell line.