- ANTAGONISTS OF THE TOLL-LIKE RECEPTOR 1/2 COMPLEX
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Provided are compounds, compositions and methods for treating Toll-like receptor 1/2 complex (TLRI/2) related inflammatory disorders. Small molecules, based on the benzotropolone scaffold, capable of influencing downstream signaling are dislcosed as well as methods of making and modifying these molecules. Also provided are methods for treating a subject for a clinical condition associated with Toll? like receptor complex 1/2 activation, comprising administering to the subject an effective amount of a benzotropolone compound.
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Page/Page column 18; 19; 21
(2014/02/16)
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- Synthesis and evaluation as potential anticancer agents of novel tetracyclic indenoquinoline derivatives
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We report the synthesis and evaluation as potential anticancer agents of a series of tetracyclic indenoquinolines. The compounds, which are obtained through the photoisomerization of Diels-Alder adducts formed between purpurogallin derivatives and nitrosobenzene, have in vitro antiproliferative activities in the μM to nM range against breast (MCF-7), lung epithelial (A-549), and cervical (HeLa) adenocarcinoma cells. The cytotoxicities of several of the novel tetracycles are comparable to or better than that of camptothecin. A strong correlation between the activity of the compounds and their aromaticity and planarity was observed, suggesting a mode of action similar to that of topoisomerase poisons.
- Chakrabarty, Shubhashis,Croft, Michael S.,Marko, Melissa G.,Moyna, Guillermo
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p. 1143 - 1149
(2013/03/28)
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- Discovery of small-molecule inhibitors of the TLR1/TLR2 complex
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An important regulator of innate immunity, the protein complex of Toll-like receptors 1 and 2 (TLR1/TLR2) provides an attractive target for the treatment of various immune disorders. The novel compound CU-CPT22 can compete with the binding of the specific lipoprotein ligand to TLR1/TLR2 (see picture) with high inhibitory activity and specificity. Repression of downstream signaling from TNF-α and IL-1β was also observed. Copyright
- Cheng, Kui,Wang, Xiaohui,Zhang, Shuting,Yin, Hang
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supporting information
p. 12246 - 12249
(2013/02/23)
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- Synthesis and in vitro protozoocidal activity of diazabicyclic benzotropolone derivatives
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We describe the synthesis and protozoocidal evaluation of a series of diazabicycles based on benzotropolone ethers. Several of the compounds, which can be obtained through a high-yielding hetero Diels-Alder reaction using simple and readily available star
- Khrizman, Alexander,Moulthrop, Jason S.,Little, Susan,Wharton, Hayley,Yardley, Vanessa,Moyna, Guillermo
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p. 4183 - 4186
(2008/03/11)
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- Synthesis and biological evaluation of O-alkylated tropolones and related α-ketohydroxy derivatives as ribonucleotide reductase inhibitors
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A series of O-alkylated tropolones and related α-ketohydroxy compounds were evaluated for their biological activities and were shown to present an expected ribonucleotide reductase inhibition and cytotoxicity against some cancer cell lines but no antitubulin activity. Pharmacomodulation studies were realised to understand and enhance the observed activities. These original benzylic, heterocyclic and allylic compounds have been synthesised by a phase-transfer catalysed O-alkylation developed in our laboratories.
- Tamburlin-Thumin, Isabelle,Crozet, Michel P.,Barriere, Jean-Claude,Barreau, Michel,Riou, Jean-Francois,Lavelle, Francois
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p. 561 - 568
(2007/10/03)
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