- Indolamide compound with anti-tumor activity
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The invention discloses an indolamide compound with anti-tumor activity, which can be used for treating cancers, particularly gastric cancer, liver cancer, breast cancer, lung cancer cells and cervical cancer, and is particularly used for inhibiting human gastric cancer cells MGC-803, human liver cancer cells HepG2, human breast cancer cells MCF-7, human lung cancer cells A549 and human cervical cancer cell HELA cell strain. Therefore, the indolamide compound with anti-tumor activity can be used as a broad-spectrum anti-tumor drug, and has a good development and application prospect.
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Paragraph 0039; 0043
(2019/01/07)
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- N6-Substituted Adenosine Receptor Agonists. Synthesis and Pharmacological Activity as Potent Antinociceptive Agents
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Novel N6-(indol-3-yl)alkyl derivatives of adenosine were synthesized.The adenosine receptor affinity and the antinociceptive activity of these compounds were assessed in binding studies and the phenylbenzoquinone-induced writhing test.Most of these analogues exhibited a potent analgesic activity without side effects.Among them, compound 3c (UP 202-32) bound to A1 (Ki = 110 nM) and A2 (Ki = 350 nM) adenosine receptors in a specific manner since it did not interact with many other receptors, especially opioid binding sites.The antinociceptive activity in the phenylbenzoquinone assay (ED50 = 3.3 mg/kg po) was antagonized by 8-cyclopentyltheophylline, suggesting that an adenosinergic mechanism underlies the analgesic activity observed with this compound.The data obtained with these new N6-substituted adenosine receptor agonists emphasize the interest of such compounds in the treatment of pain.
- Guengoer, Timur,Malabre, Patrice,Teulon, Jean-Marie,Camborde, Francoise,Meignen, Joelle,et al.
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p. 4307 - 4316
(2007/10/02)
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