Bioorganic and Medicinal Chemistry Letters p. 153 - 158 (2005)
Update date:2022-08-05
Topics: Optimization Biological testing Structure-Activity Relationship (SAR) Analysis Retrosynthetic analysis Purification and characterization Virtual Screening Regulatory Approval Scale-Up and Formulation Target Identification Safety and Toxicology Studies
Wang, Gary T.
Wang, Xilu
Wang, Weibo
Hasvold, Lisa A.
Sullivan, Gerry
Hutchins, Charles W.
O'Conner, Steve
Gentiles, Robert
Sowin, Thomas
Cohen, Jerry
Gu, Wen-Zhen
Zhang, Haiying
Rosenberg, Saul H.
Sham, Hing L.
A non-methionine FT inhibitor lead structure (1) was designed through computer modeling of the peptidomimetic FT inhibitor ABT839. Optimization of this lead resulted in compounds 2e and 2g, with FT IC50 values of 1.3 and 1.8 nM, GGT IC50 of 1400 nM, and EC50 (Ras processing) values of 13 and 11 nM, respectively.
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