Design and synthesis of pyrrolobenzodiazepine-gallic hybrid agents as p53-dependent and -independent apoptogenic signaling in melanoma cells
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- 作者：Yu-Wei Choua ; Gopal Chandru Senadib ; Chung-Yu Chenc ; Kung-Kai Kuod ; Ying-Ting Lina ; Jeh-Jeng Wangb ; Jia-Hau Leeb ; Ya-Ching Wanga ; Wan-Ping Hua ; wphu@kmu.edu.tw" class="auth_mail" title="E-mail the corresponding author
- 关键词：Pyrrolobenzodiazepine ; Mitochondria ; Gallic acid ; Antitumor ; Free radical ; Melanoma
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：15 February 2016
- 年：2016
- 卷：109
- 期：Complete
- 页码：59-74
- 全文大小：3311 K
文摘
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PBD-GA hybrid agents conjugated with alkyl spacers has been designed and synthesized.
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The PBD-GA agents (5a–5d) were potently cytotoxic in A375 and RPMI7951 melanoma cells.
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PBD-GA induced p53-dependent mitochondrial apoptosis in melanoma A375 cells.
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PBD-GA induced p53-independent mitochondrial apoptosis in melanoma RPMI7951 via LMP.
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Compound 5b shown to reduce murine melanoma size in a mouse model.