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Your search keyword '"Zhu, Yongbao"' showing total 8 results
Start Over Author "Zhu, Yongbao" Publisher elsevier b.v.
8 results on '"Zhu, Yongbao"'

5. Inhibition of the cathepsin cysteine proteases B and K by square-planar cycloaurated gold(III) compounds and investigation of their anti-cancer activity

Author

Zhu, Yongbao, Cameron, Beth R., Mosi, Renee, Anastassov, Virginia, Cox, Jennifer, Qin, Ling, Santucci, Zefferino, Metz, Markus, Skerlj, Renato T., and Fricker, Simon P.

Subjects
*COLLOIDAL gold, *PROTEOLYTIC enzymes, *ANTINEOPLASTIC agents, *THIOLS, *CYSTEINE proteinases, *COLON tumors
Abstract

Abstract: Gold(III) compounds have been examined for potential anti-cancer activity. It is proposed that the molecular targets of these compounds are thiol-containing biological molecules such as the cathepsin cysteine proteases. These enzymes have been implicated in many diseases including cancer. The catalytic mechanism of the cathepsin cysteine proteases is dependent upon a cysteine at the active site which is accessible to the interaction of thiophilic metals such as gold. The synthesis and biological activity of square-planar six-membered cycloaurated Au(III) compounds with a pyridinyl-phenyl linked backbone and two monodentate or one bidentate leaving group is described. Gold(III) cycloaurated compounds were able to inhibit both cathepsins B and K. Structure/activity was investigated by modifications to the pyridinyl-phenyl backbone, and leaving groups. Optimal activity was seen with substitution at the 6 position of the pyridine ring. The reversibility of inhibition was tested by reactivation in the presence of cysteine with a bidentate thiosalicylate compound being an irreversible inhibitor. Five compounds were evaluated for in vitro cytotoxicity against a panel of human tumor cell lines. The thiosalicylate compound was tested in vivo against the HT29 human colon tumor xenograft model. A modest decrease in tumor growth was observed compared with the untreated control tumor. [Copyright &y& Elsevier]

Published
2011
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6. Design and synthesis of pyridin-2-ylmethylaminopiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication

Author

Skerlj, Renato, Bridger, Gary, Zhou, Yuanxi, Bourque, Elyse, McEachern, Ernest, Langille, Jonathan, Harwig, Curtis, Veale, Duane, Yang, Wen, Li, Tongshong, Zhu, Yongbao, Bey, Michael, Baird, Ian, Sartori, Michael, Metz, Markus, Mosi, Renee, Nelson, Kim, Bodart, Veronique, Wong, Rebecca, and Fricker, Simon

Subjects
*PYRIDINE, *DRUG design, *ANTIVIRAL agents, *HIV infections, *PROTEIN binding, *GLYCOPROTEINS, *PHARMACOKINETICS
Abstract

Abstract: A series of CCR5 antagonists were optimized for potent inhibition of R5 HIV-1 replication in peripheral blood mononuclear cells. Compounds that met acceptable ADME criteria, selectivity, human plasma protein binding, potency shift in the presence of α-glycoprotein were evaluated in rat and dog pharmacokinetics. [Copyright &y& Elsevier]

Published
2011
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7. Design of novel CXCR4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication

Author

Skerlj, Renato, Bridger, Gary, McEachern, Ernest, Harwig, Curtis, Smith, Chris, Kaller, Alan, Veale, Duane, Yee, Helen, Skupinska, Krystyna, Wauthy, Rossana, Wang, Letian, Baird, Ian, Zhu, Yongbao, Burrage, Kate, Yang, Wen, Sartori, Michael, Huskens, Dana, Clercq, Erik De, and Schols, Dominique

Subjects
*DRUG design, *CHEMOKINES, *ENZYME inhibitors, *VIRAL replication, *ANTI-HIV agents, *DRUG synergism, *STRUCTURE-activity relationships, *HIV infections, *PHARMACOKINETICS, *LABORATORY rats, *LABORATORY dogs
Abstract

Abstract: A novel series of CXCR4 antagonists were identified based on the substantial redesign of AMD070. These compounds possessed potent anti-HIV-1 activity and showed excellent pharmacokinetics in rat and dog. [Copyright &y& Elsevier]

Published
2011
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8. Synthesis and SAR of novel CXCR4 antagonists that are potent inhibitors of T tropic (X4) HIV-1 replication

Author

Skerlj, Renato, Bridger, Gary, McEachern, Ernie, Harwig, Curtis, Smith, Chris, Wilson, Trevor, Veale, Duane, Yee, Helen, Crawford, Jason, Skupinska, Krystyna, Wauthy, Rossana, Yang, Wen, Zhu, Yongbao, Bogucki, David, Di Fluri, Maria, Langille, Jonathon, Huskens, Dana, De Clercq, Erik, and Schols, Dominique

Subjects
*ENZYME inhibitors, *HIV, *VIRAL replication, *HETEROCYCLIC compounds, *CHEMOKINES, *PHARMACOKINETICS, *STRUCTURE-activity relationships
Abstract

Abstract: An early lead from the AMD070 program was optimized and a structure–activity relationship was developed for a novel series of heterocyclic containing compounds. Potent CXCR4 antagonists were identified based on anti-HIV-1 activity and Ca2+ flux inhibition that displayed good pharmacokinetics in rat and dog. [Copyright &y& Elsevier]

Published
2011
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