Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents
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- 作者：Mohsine Driowyaa ; b ; Julien Leclercqa ; b ; Valerie Veronesa ; b ; Amé ; lie Barczyka ; c ; Marie Lecoeura ; d ; Nicolas Renaulta ; c ; Nathalie Flouqueta ; b ; Alina Ghineta ; e ; Pascal Berthelota ; b ; Nicolas Lebeguea ; b ; nicolas.lebegue@univ-lille2.fr" class="auth_mail" title="E-mail the corresponding author
- 关键词：Triazoloquinazolinone ; Combretastatin ; Tubulin polymerization ; Cytotoxicity ; Antivascular
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：10 June 2016
- 年：2016
- 卷：115
- 期：Complete
- 页码：393-405
- 全文大小：2163 K
文摘
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1-phenyl-triazoloquinazolinone is considered as a conformationally restricted CA-4 analogue.
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A 3-hydroxy-4-methoxyphenyl group and N-methyl substitution are essentials for activity.
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Compound 12d displays potent anti-tubulin, cytotoxic and anti-vascular activities.