- A modified Cu(0)-Cu(I)-mediated Caryl-CarylUllmann coupling for the synthesis of biaryls
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A novel Cu(0)-Cu(I)-mediated Caryl-CarylUllmann coupling has been successfully developed. The use of Cu(I) salts allowed the reactions to proceed under relatively mild conditions (65?°C in DMSO for 15–72?h). The developed method was compatible with a relatively wide range of functional groups simultaneously present on the aromatic ring of different electronic nature. The aryl halides with an electron-withdrawing group ortho to the halide or an electron-donating group meta or para to the halide furnished the corresponding products in good to excellent yields (up to 98%).
- Yasamut, Kittisak,Jongcharoenkamol, Jira,Ruchirawat, Somsak,Ploypradith, Poonsakdi
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p. 5994 - 6000
(2016/09/14)
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- Exploring the formation and recognition of an important G-quadruplex in a HIF1α promoter and its transcriptional inhibition by a benzo[c]phenanthridine derivative
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Four putative G-quadruplex sequences (PGSs) in the HIF1α promoter and the 5′UTR were evaluated for their G-quadruplex-forming potential using ESI-MS, CD, FRET, DMS footprinting, and a polymerase stop assay. An important G-quadruplex (S1) has been proven to inhibit HIF1α transcription by blocking AP2 binding. A benzo[c]phenanthridine derivative was found to target the S1 G-quadruplex and induce its conformational conversion from antiparallel to parallel orientation. The transcriptional suppression of HIF1α by this compound was demonstrated using western blotting, Q-RT-PCR, luciferase assay, and ChIP. Our new findings provided a novel strategy for HIF1α regulation and potential insight for cancer therapy.
- Chen, Han,Long, Haitao,Cui, Xiaojie,Zhou, Jiang,Xu, Ming,Yuan, Gu
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supporting information
p. 2583 - 2591
(2014/03/21)
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- Synthesis of The Diaza Analogue of Ellagic Acid
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The novel diaza analogue 2 of DNA-gyrase inhibitor ellagic acid 1 was synthesized via the Ullmann coupling of methyl 2-bromo-3-nitroveratrate 6 which, in turn, was prepared by a 7-step synthesis from 2-bromopiperonal 10 requiring a contrived, regiospecifi
- Kanojia, Ramesh M.,Ohemeng, Kwasi A.,Schwender, Charles F.,Barrett, John F.
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p. 8553 - 8556
(2007/10/02)
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