Journal of Medicinal Chemistry p. 3368 - 3385 (2011)
Update date:2022-08-05
Topics:
Zehnder, Luke
Bennett, Michael
Meng, Jerry
Huang, Buwen
Ninkovic, Sacha
Wang, Fen
Braganza, John
Tatlock, John
Jewell, Tanya
Zhou, Joe Zhongxiang
Burke, Ben
Wang, Jeff
Maegley, Karen
Mehta, Pramod P.
Yin, Min-Jean
Gajiwala, Ketan S.
Hickey, Michael J.
Yamazaki, Shinji
Smith, Evan
Kang, Ping
Sistla, Anand
Dovalsantos, Elena
Gehring, Michael R.
Kania, Robert
Wythes, Martin
Kung, Pei-Pei
Figure Presented. A novel class of heat shock protein 90 (Hsp90) inhibitors was discovered by high-throughput screening and was subsequently optimized using a combination of structure-based design, parallel synthesis, and the application of medicinal chemistry principles. Through this process, the biochemical and cell-based potency of the original HTS lead were substantially improved along with the corresponding metabolic stability properties. These efforts culminated with the identification of a development candidate (compound 42) which displayed desired PK/PD relationships, significant efficacy in a melanoma A2058 xenograft tumor model, and attractive DMPK profiles.
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Doi:10.1039/jr9440000571
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(2011)Doi:10.1039/c3sc51616d
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(2011)Doi:10.1021/jm00106a004
(1991)