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8 results on '"Cao, Benjamin"'

2. Validating Eaton's Hypothesis: Cubane as a Benzene Bioisostere.

Author

Chalmers, Benjamin A., Xing, Hui, Houston, Sevan, Stok, Jeanette E., Bernhardt, Paul V., De Voss, James J., Williams, Craig M., Clark, Charlotte, Cooper, Helen M., Ghassabian, Sussan, Kuo, Andy, Smith, Maree T., Littler, Stuart W., Tsanaktsidis, John, Savage, G. Paul, Cao, Benjamin, Reitsma, Andrea, Nilsson, Susan K., Winkler, David A., and Murray, Cody-Ellen P.

Subjects
CUBANES, BIOISOSTERES, BENZENE, CELL transplantation, HISTONE deacetylase inhibitors
Abstract

Pharmaceutical and agrochemical discovery programs are under considerable pressure to meet increasing global demand and thus require constant innovation. Classical hydrocarbon scaffolds have long assisted in bringing new molecules to the market place, but an obvious omission is that of the Platonic solid cubane. Eaton, however, suggested that this molecule has the potential to act as a benzene bioisostere. Herein, we report the validation of Eaton's hypothesis with cubane derivatives of five molecules that are used clinically or as agrochemicals. Two cubane analogues showed increased bioactivity compared to their benzene counterparts whereas two further analogues displayed equal bioactivity, and the fifth one demonstrated only partial efficacy. Ramifications from this study are best realized by reflecting on the number of bioactive molecules that contain a benzene ring. Substitution with the cubane scaffold where possible could revitalize these systems, and thus expedite much needed lead candidate identification. [ABSTRACT FROM AUTHOR]

Published
2016
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4. Corrigendum: Validating Eaton's Hypothesis: Cubane as a Benzene Bioisostere.

Author

Chalmers, Benjamin A., Xing, Hui, Houston, Sevan, Clark, Charlotte, Ghassabian, Sussan, Kuo, Andy, Cao, Benjamin, Reitsma, Andrea, Murray, Cody‐Ellen P., Stok, Jeanette E., Boyle, Glen M., Pierce, Carly J., Littler, Stuart W., Winkler, David A., Bernhardt, Paul V., Pasay, Cielo, De Voss, James J., McCarthy, James, Parsons, Peter G., and Walter, Gimme H.

Subjects
HYPOTHESIS, BENZENE, BIOISOSTERES
Published
2018
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5. Berichtigung: Validating Eaton's Hypothesis: Cubane as a Benzene Bioisostere.

Author

Chalmers, Benjamin A., Xing, Hui, Houston, Sevan, Clark, Charlotte, Ghassabian, Sussan, Kuo, Andy, Cao, Benjamin, Reitsma, Andrea, Murray, Cody‐Ellen P., Stok, Jeanette E., Boyle, Glen M., Pierce, Carly J., Littler, Stuart W., Winkler, David A., Bernhardt, Paul V., Pasay, Cielo, De Voss, James J., McCarthy, James, Parsons, Peter G., and Walter, Gimme H.

Subjects
CUBANES, BENZENE, BIOISOSTERES
Published
2018
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7. Frontispiece: Validating Eaton's Hypothesis: Cubane as a Benzene Bioisostere.

Author

Chalmers, Benjamin A., Xing, Hui, Houston, Sevan, Stok, Jeanette E., Bernhardt, Paul V., De Voss, James J., Williams, Craig M., Clark, Charlotte, Cooper, Helen M., Ghassabian, Sussan, Kuo, Andy, Smith, Maree T., Littler, Stuart W., Tsanaktsidis, John, Savage, G. Paul, Cao, Benjamin, Reitsma, Andrea, Nilsson, Susan K., Winkler, David A., and Murray, Cody-Ellen P.

Subjects
FRONTISPIECE, BIOISOSTERES
Abstract

The cover page of the journal “Angewandte Chemie" is presented.

Published
2016
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