Potent Farnesyltransferase Inhibitors with 1,4-Diazepane Scaffolds as Novel Destabilizing Microtubule Agents in Hormone-Resistant Prostate Cancer

Journal of Medicinal Chemistry
2011.0

Abstract

A new class of potent farnesyltransferase inhibitors based on a 1,4-diazepane scaffold was synthesized with protein farnesyltransferase inhibition potencies in the low nanomolar range. The compounds block the growth on two hormone-resistant tumor prostatic cell lines (DU145 and PC3). The advanced cellular evaluation of the more potent farnesyltransferase inhibitors was explored and revealed a disorganization of tubulin in PC3 cells.

Knowledge Graph

Similar Paper

Potent Farnesyltransferase Inhibitors with 1,4-Diazepane Scaffolds as Novel Destabilizing Microtubule Agents in Hormone-Resistant Prostate Cancer
Journal of Medicinal Chemistry 2011.0
Identification of Pharmacokinetically Stable 3,10-Dibromo-8-chlorobenzocycloheptapyridine Farnesyl Protein Transferase Inhibitors with Potent Enzyme and Cellular Activities
Journal of Medicinal Chemistry 1999.0
Potent and Selective Farnesyl Transferase Inhibitors
Journal of Medicinal Chemistry 2004.0
Synthesis, biological evaluation and SAR of naftopidil-based arylpiperazine derivatives
Bioorganic & Medicinal Chemistry Letters 2018.0
Design, Synthesis, and Biological Activity of 4-[(4-Cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles as Potent and Selective Farnesyltransferase Inhibitors
Journal of Medicinal Chemistry 2004.0
Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors
Bioorganic & Medicinal Chemistry Letters 2005.0
Design, synthesis, and activity of 4-quinolone and pyridone compounds as nonthiol-containing farnesyltransferase inhibitors
Bioorganic & Medicinal Chemistry Letters 2004.0
Design, synthesis and biological evaluation of pyridine-chalcone derivatives as novel microtubule-destabilizing agents
European Journal of Medicinal Chemistry 2019.0
New (3-(1H-benzo[d]imidazol-2-yl))/(3-(3H-imidazo[4,5-b]pyridin-2-yl))-(1H-indol-5-yl)(3,4,5-trimethoxyphenyl)methanone conjugates as tubulin polymerization inhibitors
MedChemComm 2017.0
Design, Synthesis, and Preclinical Evaluation of 4-Substituted-5-methyl-furo[2,3-d]pyrimidines as Microtubule Targeting Agents That Are Effective against Multidrug Resistant Cancer Cells
Journal of Medicinal Chemistry 2016.0