Výsledky vyhledávání - "Howard S. Roth"

Small-Molecule Procaspase-3 Activation Sensitizes Cancer to Treatment with Diverse Chemotherapeutics

Autor: Howard S. Roth, Rachel C. Botham, Paul J. Hergenrother, Timothy M. Fan, Alison P. Book, Patrick J. Roady

Publikováno v: ACS Central Science, Vol 2, Iss 8, Pp 545-559 (2016)
ACS Central Science

Conventional chemotherapeutics remain essential treatments for most cancers, but their combination with other anticancer drugs (including targeted therapeutics) is often complicated by unpredictable synergies and multiplicative toxicities. As cytotox

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f10efed789326fa7157f3b0e15b4d1f
https://doi.org/10.1021/acscentsci.6b00165

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Synthesis of [5,6]-Bicyclic Heterocycles with a Ring-Junction Nitrogen via Rh(III)-Catalyzed C-H Functionalization of Alkenyl Azoles

Autor: Howard S. Roth, Jonathan A. Ellman, Kim Søholm Halskov

The first syntheses of privileged [5,6]-bicyclic heterocycles, with ring-junction nitrogen atoms, by transition metal catalyzed C-H functionalization of C-alkenyl azoles is disclosed. Several reactions are applied to alkenyl imidazoles, pyrazoles, an

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4a68b5f36f87da7de9eb8da2fb5eb27b
https://europepmc.org/articles/PMC5564303/

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Derivatives of Procaspase-Activating Compound 1 (PAC-1) and Anticancer Activities

Autor: Howard S. Roth, Paul J. Hergenrother

PAC-1 induces the activation of procaspase-3 in vitro and in cell culture by chelation of inhibitory labile zinc ions via its ortho-hydroxy-N-acylhydrazone moiety. First reported in 2006, PAC-1 has shown promise in cell culture and animal models of c

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0e825688ca1b14f94206b5abc2957b6a
https://europepmc.org/articles/PMC4968085/

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Parallel Synthesis and Biological Evaluation of 837 Analogues of Procaspase-Activating Compound 1 (PAC-1)

Autor: Rachel C. Botham, Steven C. Schmid, Danny Chung Hsu, Chris J. Novotny, Howard S. Roth, Paul J. Hergenrother, Diana C. West

Publikováno v: ACS Combinatorial Science. 14:44-50

Procaspase-Activating Compound 1 (PAC-1) is an ortho-hydroxy N-acyl hydrazone that enhances the enzymatic activity of procaspase-3 in vitro and induces apoptosis in cancer cells. An analogue of PAC-1, called S-PAC-1, was evaluated in a veterinary cli

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7048f4823d41901014a0dcff440a7f6a
https://doi.org/10.1021/co2001372

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Removal of Metabolic Liabilities Enables Development of Derivatives of Procaspase-Activating Compound 1 (PAC-1) with Improved Pharmacokinetics

Autor: Howard S. Roth, Levent Dirikolu, Steven C. Schmid, Rachel C. Botham, Paul J. Hergenrother, Timothy M. Fan

Procaspase-activating compound 1 (PAC-1) is an o-hydroxy-N-acylhydrazone that induces apoptosis in cancer cells by chelation of labile inhibitory zinc from procaspase-3. PAC-1 has been assessed in a wide variety of cell culture experiments and in viv

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::545720c5f996953b9a9cd1b100214495
https://europepmc.org/articles/PMC4520234/

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N-heterocyclic carbene-catalyzed rearrangements of vinyl sulfones

Autor: Roxanne L. Atienza, Howard S. Roth, Karl A. Scheidt

Publikováno v: Chemical science. 2(9)

N-heterocyclic carbenes catalyze the rearrangement of 1,1-bis(arylsulfonyl)ethylene to the corresponding trans-1,2-bis(phenylsulfonyl) under mild conditions. Tandem rearrangement/cycloadditions have been developed to capitalize on this new process an

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c7141eb30921a62002460c7613b3fe46
https://pubmed.ncbi.nlm.nih.gov/22448316

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