-transparent.png){kind=logo}
The design, synthesis, and biological evaluation of PIM kinase inhibitors. 2012
Amy Lew Tsuhako, and
David S Brown, and
Elena S Koltun, and
Naing Aay, and
Arlyn Arcalas, and
Vicky Chan, and
Hongwang Du, and
Stefan Engst, and
Maurizio Franzini, and
Adam Galan, and
Ping Huang, and
Stuart Johnston, and
Brian Kane, and
Moon H Kim, and
A Douglas Laird, and
Rui Lin, and
Lillian Mock, and
Iris Ngan, and
Michael Pack, and
Gordon Stott, and
Thomas J Stout, and
Peiwen Yu, and
Cristiana Zaharia, and
Wentao Zhang, and
Peiwen Zhou, and
John M Nuss, and
Patrick C Kearney, and
Wei Xu
Exelixis, Department of Drug Discovery, South San Francisco, CA 94080, USA. alew@exelixis.com
A series of substituted benzofuropyrimidinones with pan-PIM activities and excellent selectivity against a panel of diverse kinases is described. Initial exploration identified aryl benzofuropyrimidinones that were potent, but had cell permeability limitation. Using X-ray crystal structures of the bound PIM-1 complexes with 3, 5m, and 6d, we were able to guide the SAR and identify the alkyl benzofuropyrimidinone (6l) with good PIM potencies, permeability, and oral exposure.
Related Publications
Amy Lew Tsuhako, and
David S Brown, and
Elena S Koltun, and
Naing Aay, and
Arlyn Arcalas, and
Vicky Chan, and
Hongwang Du, and
Stefan Engst, and
Maurizio Franzini, and
Adam Galan, and
Ping Huang, and
Stuart Johnston, and
Brian Kane, and
Moon H Kim, and
A Douglas Laird, and
Rui Lin, and
Lillian Mock, and
Iris Ngan, and
Michael Pack, and
Gordon Stott, and
Thomas J Stout, and
Peiwen Yu, and
Cristiana Zaharia, and
Wentao Zhang, and
Peiwen Zhou, and
John M Nuss, and
Patrick C Kearney, and
Wei Xu
February 2021,
Molecules (Basel, Switzerland),
Amy Lew Tsuhako, and
David S Brown, and
Elena S Koltun, and
Naing Aay, and
Arlyn Arcalas, and
Vicky Chan, and
Hongwang Du, and
Stefan Engst, and
Maurizio Franzini, and
Adam Galan, and
Ping Huang, and
Stuart Johnston, and
Brian Kane, and
Moon H Kim, and
A Douglas Laird, and
Rui Lin, and
Lillian Mock, and
Iris Ngan, and
Michael Pack, and
Gordon Stott, and
Thomas J Stout, and
Peiwen Yu, and
Cristiana Zaharia, and
Wentao Zhang, and
Peiwen Zhou, and
John M Nuss, and
Patrick C Kearney, and
Wei Xu
May 2018,
Bioorganic & medicinal chemistry,
Amy Lew Tsuhako, and
David S Brown, and
Elena S Koltun, and
Naing Aay, and
Arlyn Arcalas, and
Vicky Chan, and
Hongwang Du, and
Stefan Engst, and
Maurizio Franzini, and
Adam Galan, and
Ping Huang, and
Stuart Johnston, and
Brian Kane, and
Moon H Kim, and
A Douglas Laird, and
Rui Lin, and
Lillian Mock, and
Iris Ngan, and
Michael Pack, and
Gordon Stott, and
Thomas J Stout, and
Peiwen Yu, and
Cristiana Zaharia, and
Wentao Zhang, and
Peiwen Zhou, and
John M Nuss, and
Patrick C Kearney, and
Wei Xu
August 2012,
Bioorganic & medicinal chemistry letters,
Amy Lew Tsuhako, and
David S Brown, and
Elena S Koltun, and
Naing Aay, and
Arlyn Arcalas, and
Vicky Chan, and
Hongwang Du, and
Stefan Engst, and
Maurizio Franzini, and
Adam Galan, and
Ping Huang, and
Stuart Johnston, and
Brian Kane, and
Moon H Kim, and
A Douglas Laird, and
Rui Lin, and
Lillian Mock, and
Iris Ngan, and
Michael Pack, and
Gordon Stott, and
Thomas J Stout, and
Peiwen Yu, and
Cristiana Zaharia, and
Wentao Zhang, and
Peiwen Zhou, and
John M Nuss, and
Patrick C Kearney, and
Wei Xu
December 2018,
Bioorganic & medicinal chemistry letters,
Amy Lew Tsuhako, and
David S Brown, and
Elena S Koltun, and
Naing Aay, and
Arlyn Arcalas, and
Vicky Chan, and
Hongwang Du, and
Stefan Engst, and
Maurizio Franzini, and
Adam Galan, and
Ping Huang, and
Stuart Johnston, and
Brian Kane, and
Moon H Kim, and
A Douglas Laird, and
Rui Lin, and
Lillian Mock, and
Iris Ngan, and
Michael Pack, and
Gordon Stott, and
Thomas J Stout, and
Peiwen Yu, and
Cristiana Zaharia, and
Wentao Zhang, and
Peiwen Zhou, and
John M Nuss, and
Patrick C Kearney, and
Wei Xu
October 2011,
Journal of medicinal chemistry,
Amy Lew Tsuhako, and
David S Brown, and
Elena S Koltun, and
Naing Aay, and
Arlyn Arcalas, and
Vicky Chan, and
Hongwang Du, and
Stefan Engst, and
Maurizio Franzini, and
Adam Galan, and
Ping Huang, and
Stuart Johnston, and
Brian Kane, and
Moon H Kim, and
A Douglas Laird, and
Rui Lin, and
Lillian Mock, and
Iris Ngan, and
Michael Pack, and
Gordon Stott, and
Thomas J Stout, and
Peiwen Yu, and
Cristiana Zaharia, and
Wentao Zhang, and
Peiwen Zhou, and
John M Nuss, and
Patrick C Kearney, and
Wei Xu
October 2009,
Journal of medicinal chemistry,
Amy Lew Tsuhako, and
David S Brown, and
Elena S Koltun, and
Naing Aay, and
Arlyn Arcalas, and
Vicky Chan, and
Hongwang Du, and
Stefan Engst, and
Maurizio Franzini, and
Adam Galan, and
Ping Huang, and
Stuart Johnston, and
Brian Kane, and
Moon H Kim, and
A Douglas Laird, and
Rui Lin, and
Lillian Mock, and
Iris Ngan, and
Michael Pack, and
Gordon Stott, and
Thomas J Stout, and
Peiwen Yu, and
Cristiana Zaharia, and
Wentao Zhang, and
Peiwen Zhou, and
John M Nuss, and
Patrick C Kearney, and
Wei Xu
April 2016,
Bioorganic & medicinal chemistry,
Amy Lew Tsuhako, and
David S Brown, and
Elena S Koltun, and
Naing Aay, and
Arlyn Arcalas, and
Vicky Chan, and
Hongwang Du, and
Stefan Engst, and
Maurizio Franzini, and
Adam Galan, and
Ping Huang, and
Stuart Johnston, and
Brian Kane, and
Moon H Kim, and
A Douglas Laird, and
Rui Lin, and
Lillian Mock, and
Iris Ngan, and
Michael Pack, and
Gordon Stott, and
Thomas J Stout, and
Peiwen Yu, and
Cristiana Zaharia, and
Wentao Zhang, and
Peiwen Zhou, and
John M Nuss, and
Patrick C Kearney, and
Wei Xu
December 2011,
ACS medicinal chemistry letters,
Amy Lew Tsuhako, and
David S Brown, and
Elena S Koltun, and
Naing Aay, and
Arlyn Arcalas, and
Vicky Chan, and
Hongwang Du, and
Stefan Engst, and
Maurizio Franzini, and
Adam Galan, and
Ping Huang, and
Stuart Johnston, and
Brian Kane, and
Moon H Kim, and
A Douglas Laird, and
Rui Lin, and
Lillian Mock, and
Iris Ngan, and
Michael Pack, and
Gordon Stott, and
Thomas J Stout, and
Peiwen Yu, and
Cristiana Zaharia, and
Wentao Zhang, and
Peiwen Zhou, and
John M Nuss, and
Patrick C Kearney, and
Wei Xu
December 2021,
Bioorganic & medicinal chemistry letters,
Amy Lew Tsuhako, and
David S Brown, and
Elena S Koltun, and
Naing Aay, and
Arlyn Arcalas, and
Vicky Chan, and
Hongwang Du, and
Stefan Engst, and
Maurizio Franzini, and
Adam Galan, and
Ping Huang, and
Stuart Johnston, and
Brian Kane, and
Moon H Kim, and
A Douglas Laird, and
Rui Lin, and
Lillian Mock, and
Iris Ngan, and
Michael Pack, and
Gordon Stott, and
Thomas J Stout, and
Peiwen Yu, and
Cristiana Zaharia, and
Wentao Zhang, and
Peiwen Zhou, and
John M Nuss, and
Patrick C Kearney, and
Wei Xu
October 2012,
European journal of medicinal chemistry,
