Synthesis, structure elucidation, DNA-PK and PI3K and anti-cancer activity of 8- and 6-aryl-substituted-1-3-benzoxazines
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- 作者：Rick Morrisona ; rmmorrison@students.latrobe.edu.au" class="auth_mail" title="E-mail the corresponding author ; Jasim M.A. Al-Rawia ; j.al-rawi@latrobe.edu.au" class="auth_mail" title="E-mail the corresponding author ; Ian G. Jenningsb ; Ian.Jennings@monash.edu" class="auth_mail" title="E-mail the corresponding author ; Philip E. Thompsonb ; Philip.Thompson@monash.edu" class="auth_mail" title="E-mail the corresponding author ; Michael J. Angovea ; m.angove@latrobe.edu.au" class="auth_mail" title="E-mail the corresponding author
- 关键词：Suzuki coupling synthesis of 8- and 6-aryl-2-morpholino-1 ; 3-benzoxazines ; DNA-PK ; PI3K ; Anti-cancer activity
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：3 March 2016
- 年：2016
- 卷：110
- 期：Complete
- 页码：326-339
- 全文大小：1299 K
文摘
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We described the synthesis of 6-aryl, 8- aryl, and -2-morpholino-benzoxazines as potent DNA-PK and selective over PI3K.
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class="boldFont">20i (8-(Naphthalen-1-yl) showed strong anti-proliferative activity (GI% at 10 µM = 92) against A498 renal cancer cells.
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class="boldFont">20k (8-Dibenzo[b,d]thiophen-4-yl) the most DNA-PK active with IC50 = 0.034 µM and 170 fold more selective over the PI3K.