Výsledky vyhledávání - "Thomas A. Rano"

Indinavir analogues with blocked metabolism sites as HIV protease inhibitors with improved pharmacological profiles and high potency against PI-Resistant viral strains

Autor: Zhijian Lu, Jiunn H. Lin, Thomas A. Rano, Fengqi Zhang, Mark Stahlhut, Lixia Jin, Lori J. Gabryelski, William A. Schleif, Emilio A. Emini, Kevin T. Chapman, Carrie A. Rutkowski, Yuan Cheng, James R. Tata, David B. Olsen

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 12:2419-2422

Indinavir analogues with blocked metabolism sites show highly improved pharmacokinetic profiles in animals. The cis-aminochromanol substituted analogues exhibited excellent potency against both the wild-type (NL4-3) virus and protease inhibitor-resis

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e9046d6fc62554fca12bc99b1661c598
https://doi.org/10.1016/s0960-894x(02)00424-9

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A Combinatorial Library of Indinavir Analogues and Its In Vitro and In Vivo Studies

Autor: Zhijian Lu, Rick C. King, James R. Tata, Fengqi Zhang, Xin Xu, Jiunn H. Lin, Kevin T. Chapman, Timothy V. Olah, Tracy Huening, Lawrennce C. Kuo, Lixia Jin, Yuan Cheng, David B. Olsen, Mark Stahlhut, William A. Schleif, Debra A. McLoughlin, Thomas A. Rano, Lori J. Gabryelski

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 12:529-532

A combinatorial library of 300HIV protease inhibitors has been synthesized. The library was screened against recombinant wild-type and mutant HIV-1 protease enzymes. The pharmacokinetics of the library was evaluated by dosing in dogs. Compounds that

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6b528f9f0b54c3d30e2c7eaf20b5a926
https://doi.org/10.1016/s0960-894x(01)00824-1

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Combinatorial diversification of indinavir: in vivo mixture dosing of an HIV protease inhibitor library

Autor: Xin Xu, Kevin T. Chapman, Tracy Huening, Thomas A. Rano, Yuan Cheng, Lawrence C. Kuo, David B. Olsen, William A. Schleif, James R. Tata, Debra A. McLoughlin, Lori J. Gabryelski, Richard King, Jiunn H. Lin, Fengqi Zhang, Timothy V. Olah

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 10:1527-1530

An efficient combination solution-phase/solid-phase route enabling the diversification of the P1', P2', and P3 subsites of indinavir has been established. The synthetic sequence can facilitate the rapid generation of HIV protease inhibitors possessin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c44e5511163c14649e4ed147f3f6580c
https://doi.org/10.1016/s0960-894x(00)00276-6

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A Combinatorial Approach Defines Specificities of Members of the Caspase Family and Granzyme B

Autor: Kevin T. Chapman, Tracy Timkey, Margarita Garcia-Calvo, Vicky M. Houtzager, Dita M. Rasper, Donald W. Nicholson, Erin P. Peterson, Nancy A. Thornberry, Thomas A. Rano, Sophie Roy, John P. Vaillancourt, Penny A. Nordstrom

Publikováno v: Journal of Biological Chemistry. 272:17907-17911

There is compelling evidence that members of the caspase (interleukin-1beta converting enzyme/CED-3) family of cysteine proteases and the cytotoxic lymphocyte-derived serine protease granzyme B play essential roles in mammalian apoptosis. Here we use

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::3014846097bb3ec6545e1dc033de57e9
https://doi.org/10.1074/jbc.272.29.17907

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Solid phase synthesis of aryl ethers via the mitsunobu reaction

Autor: Kevin T. Chapman, Thomas A. Rano

Publikováno v: Tetrahedron Letters. 36:3789-3792

A procedure for the preparation of aryl ethers on a solid support employing the Mitsunobu reaction is described. Either polymer bound phenols or benzyl alcohols react rapidly and cleanly with TMAD/Bu 3 P and the appropriate electrophile/nucleophile t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b263f47f5fa27895872623e3b1eef188
https://doi.org/10.1016/0040-4039(95)00607-e

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ChemInform Abstract: Solid-Phase Synthesis of Aryl Ethers via the Mitsunobu Reaction

Autor: Kevin T. Chapman, Thomas A. Rano

Publikováno v: ChemInform. 26

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1c9aa2fda9c3b180e758c957b7a4c7e4
https://doi.org/10.1002/chin.199549100

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Total synthesis of the cytotoxic macrocycle (+)-hitachimycin

Autor: Amos B. Smith, Noritaka Chida, John L. Wood, Gary A. Sulikowski, Thomas A. Rano

Publikováno v: Journal of the American Chemical Society. 114:8008-8022

The first total synthesis of the antitumor antibiotic (+)-hitachimycin (a.k.a. stubomycin) (1) has been achieved in 22 steps and 1.1% overall yield. The cornerstone of the synthetic strategy was a highly stereoselective three-component coupling of (-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5170eaab998770499f0051babade3be7
https://doi.org/10.1021/ja00047a008

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HIV protease inhibitors with picomolar potency against PI-Resistant HIV-1 by extension of the P3 substituent

Autor: Jiunn H. Lin, Lawrence C. Kuo, Thomas A. Rano, Emilio A. Emini, James R. Tata, Nancy J. Kevin, Carrie A. Rutkowski, Kevin T. Chapman, Mark Stahlhut, William A. Schleif, Joseph L. Duffy, David B. Olsen, Lixia Jin

Publikováno v: Bioorganicmedicinal chemistry letters. 13(15)

A biaryl pyridylfuran P 3 substituent on the hydroxyethylene isostere scaffold affords HIV protease inhibitors (PI's) with picomolar (IC 50 ) potency against the protease enzymes from PI-resistant HIV-1 strains. Inclusion of a gem-dimethyl substituen

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::13b5504bdf4ad1d604986ace859d0e32
https://pubmed.ncbi.nlm.nih.gov/12852968

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Total synthesis of (+)-hitachimycin

Autor: Noritaka Chida, Thomas A. Rano, Gary A. Sulikowski, Amos B. Smith

Publikováno v: The Journal of Organic Chemistry. 55:1136-1138

The first total synthesis of the macrocyclic antibiotic-antitumor agent (+)-hitachimycin has been achieved via a convergent and efficient route. The key transformation entailed a highly stereoselective, three-component coupling of (−)-5-methoxycycl

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::123bfed9bb5faf50a2a0cd7e495044c1
https://doi.org/10.1021/jo00291a005

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