Výsledky vyhledávání - "Hwei-Ru Tsou"

Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR)

Autor: Hwei-Ru Tsou, George Theodore Grosu, Semiramis Ayral-Kaloustian, Natasja Brooijmans, Joel Bard, Ker Yu, Matthew Gregory Bursavich, Tarek S. Mansour, Gary Harold Birnberg, Irwin Hollander, Lourdes Toral-Barza, Gloria Jean Macewan

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:2321-2325

We discovered 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR). Since phenolic OH groups pose metabolic liability, one

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::423078d3b728d24b55623b4661e9206d
https://doi.org/10.1016/j.bmcl.2010.01.135

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Palladium-catalyzed arylation of N,N-dialkylhydrazines and the subsequent conversion to anilines

Autor: Michael Barry, Hwei-Ru Tsou, Xiaoxiang Liu

Publikováno v: Tetrahedron Letters. 48:8409-8412

Palladium-catalyzed aminations of different ArBr with N , N -dialkylhydrazines are described. The reaction proceeded in moderate to excellent yield (up to 90%) with good functional groups compatibilities as cyano, ester, ketone and Boc-amine groups a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::3910e30777506e4a96058f0ff03a9999
https://doi.org/10.1016/j.tetlet.2007.09.177

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Antitumor Activity of HKI-272, an Orally Active, Irreversible Inhibitor of the HER-2 Tyrosine Kinase

Autor: Xiaoqing Shi, Bernard Dean Johnson, Carolyn Discafani, Ramaswamy Nilakantan, Edward Rosfjord, Hwei-Ru Tsou, Michelle Baxter, Allan Wissner, Ru Shen, W. A. Hallett, Marvin F Reich, M. Brawner Floyd, Elsebe Overbeek, Sridhar K. Rabindran, Yu-Fen Wang, Jonathan Golas

Publikováno v: Cancer Research. 64:3958-3965

HER-2 belongs to the ErbB family of receptor tyrosine kinases, which has been implicated in a variety of cancers. Overexpression of HER-2 is seen in 25–30% of breast cancer patients and predicts a poor outcome in patients with primary disease. Tras

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cd04b2d6d2ab228cad72dfb5623aa655
https://doi.org/10.1158/0008-5472.can-03-2868

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Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents

Autor: Hwei-Ru Tsou, Yu-Fen Wang, Ramaswamy Nilakantan, Lee M. Greenberger, M. Brawner Floyd, Ru Shen, Sridhar K. Rabindran, Allan Wissner

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 12:2893-2897

The syntheses and biological evaluations of 4-anilinoquinoline-3-carbonitrile analogues of the three clinical lead 4-anilinoquinazolines Iressa, Tarceva, and CI-1033 are described. The EGFR and HER-2 kinase inhibitory activities and the cell growth i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fbf7b0cb20b0095bd193ca3200065bf5
https://doi.org/10.1016/s0960-894x(02)00598-x

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Determination of the loading values for high levels of drugs and sugars conjugated to proteins by matrix-assisted ultraviolet laser desorption/ionization mass spectrometry

Autor: Irwin Hollander, Allan Wissner, Michael Karas, Arnd Ingendoh, Hwei-Ru Tsou, Franz Hillenkamp, Marshall M. Siegel, Baiwei Lin

Publikováno v: Biological Mass Spectrometry. 22:369-376

The loading values of high levels of anti-cancer drugs and sugars conjugated to human serum albumin were determined by matrix-assisted ultraviolet (UV) laser desorption/ionization mass spectrometry. The values were compared with those obtained by UV

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::22d4892b15948b4a26bf5289f5e58ff9
https://doi.org/10.1002/bms.1200220702

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4-Substituted-7-azaindoles bearing a ureidobenzofuranone moiety as potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR)

Autor: Irwin Hollander, Lourdes Toral-Barza, Gloria Jean Macewan, Hwei-Ru Tsou, Semiramis Ayral-Kaloustian, Gary Harold Birnberg, Natasja Brooijmans, Nan Zhang, Ker Yu

Publikováno v: Bioorganicmedicinal chemistry letters. 20(7)

A series of 5-ureidobenzofuranones was discovered as potent and selective inhibitors of mTOR with good cellular activity. Molecular modeling studies revealed several hydrogen bond interactions of the ureido group with the enzyme at the ATP-binding si

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::78539aa3dad763c47a7439150b9ef1f5
https://pubmed.ncbi.nlm.nih.gov/20188551

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4-(Phenylaminomethylene)isoquinoline-1,3(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4 (CDK4)

Autor: Tritin Tran, Mary Grillo, Hwei-Ru Tsou, Ramaswamy Nilakantan, Mercy Adufa Otteng, Gary Harold Birnberg, Sridhar K. Rabindran, Malini Ravi, M. Brawner Floyd, Semiramis Ayral-Kaloustian, Kristina M.K. Kutterer, John P. McGinnis, Marvin F Reich

Publikováno v: Journal of medicinal chemistry. 51(12)

The cyclin-dependent kinases (CDKs), as complexes with their respective partners, the cyclins, are critical regulators of cell cycle progression. Because aberrant regulations of CDK4/cyclin D1 lead to uncontrolled cell proliferation, a hallmark of ca

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f5f0510c11718f298ead900e635a93bb
https://pubmed.ncbi.nlm.nih.gov/18494457

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