Combinatorial synthesis of anilinoanthraquinone derivatives and evaluation as non-nucleotide-derived P2Y2 receptor antagonists

Stefanie Weyler; Younis Baqi; Petra Hillmann; Marko Kaulich; Andrea M. Hunder; Ingrid A. Müller; Christa E. Müller

doi:10.1016/j.bmcl.2007.10.082

Combinatorial synthesis of anilinoanthraquinone derivatives and evaluation as non-nucleotide-derived P2Y₂ receptor antagonists

Stefanie Weyler, Younis Baqi, Petra Hillmann, Marko Kaulich, Andrea M. Hunder, Ingrid A. Müller, Christa E. Müller^*

^*المؤلف المقابل لهذا العمل

نتاج البحث: المساهمة في مجلة › Article › مراجعة النظراء

54 اقتباسات (Scopus)

ملخص

A library of anilinoanthraquinone derivatives was synthesized by parallel Ullmann coupling reaction of bromaminic acid with aniline derivatives in solution using a compact parallel synthesizer. The products were purified by HPLC and evaluated as antagonists at mouse and human P2Y₂ receptors. 4-Phenylamino-substituted 1-amino-2-sulfoanthraquinones, for example, 1-amino-4-(2-methoxyphenyl)-2-sulfoanthraquinone (PSB-716), were potent P2Y₂ antagonists with IC₅₀ values in the low micromolar range.

اللغة الأصلية	English
الصفحات (من إلى)	223-227
عدد الصفحات	5
دورية	Bioorganic and Medicinal Chemistry Letters
مستوى الصوت	18
رقم الإصدار	1
المعرِّفات الرقمية للأشياء	https://doi.org/10.1016/j.bmcl.2007.10.082
حالة النشر	Published - يناير 1 2008
منشور خارجيًا	نعم

ASJC Scopus subject areas

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الوصول إلى المستند

10.1016/j.bmcl.2007.10.082

الملفات والروابط الأخرى

قم بذكر هذا

Combinatorial synthesis of anilinoanthraquinone derivatives and evaluation as non-nucleotide-derived P2Y₂ receptor antagonists. / Weyler, Stefanie; Baqi, Younis; Hillmann, Petra وآخرون.
في: Bioorganic and Medicinal Chemistry Letters, المجلد 18, رقم 1, ٠١.٠١.٢٠٠٨, صفحة 223-227.

نتاج البحث: المساهمة في مجلة › Article › مراجعة النظراء

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title = "Combinatorial synthesis of anilinoanthraquinone derivatives and evaluation as non-nucleotide-derived P2Y2 receptor antagonists",

abstract = "A library of anilinoanthraquinone derivatives was synthesized by parallel Ullmann coupling reaction of bromaminic acid with aniline derivatives in solution using a compact parallel synthesizer. The products were purified by HPLC and evaluated as antagonists at mouse and human P2Y2 receptors. 4-Phenylamino-substituted 1-amino-2-sulfoanthraquinones, for example, 1-amino-4-(2-methoxyphenyl)-2-sulfoanthraquinone (PSB-716), were potent P2Y2 antagonists with IC50 values in the low micromolar range.",

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note = "Funding Information: This work was funded by the DFG (GRK 804) and the DAAD (scholarship for Y.B.). We thank Karen Schmeling for skilfull technical assistance. ",

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AU - Kaulich, Marko

AU - Hunder, Andrea M.

AU - Müller, Ingrid A.

AU - Müller, Christa E.

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