Download Mendeley3-Substituted Quinolines as ROR gamma t Inverse Agonists.
Tanis, V.M., Venkatesan, H., Cummings, M.D., Albers, M., Kent Barbay, J., Herman, K., Kummer, D.A., Milligan, C., Nelen, M.I., Nishimura, R., Schlueter, T., Scott, B., Spurlino, J., Wolin, R., Woods, C., Xue, X., Edwards, J.P., Fourie, A.M., Leonard, K.(2019) Bioorg Med Chem Lett 29: 1463-1470
- PubMed: 31010722
- DOI: https://doi.org/10.1016/j.bmcl.2019.04.021
- Primary Citation of Related Structures:
6NAD - PubMed Abstract:
We have previously reported the syntheses of a series of 3,6-disubstituted quinolines as modulators of the retinoic acid receptor-related orphan receptor gamma t (RORγt). These molecules are potent binders but are high molecular weight and they exhibited poor solubility at pH 2 and pH 7. This manuscript details our efforts at improving physical chemical properties for this series of compounds by increasing the diversity at the 3-position (i.e. introducing heteroatoms and lowering the molecular weight). These efforts have led to molecules which are potent binders with improved solubility.
Organizational Affiliation:
Discovery Product Development and Supply, Janssen Research and Development, 3210 Merryfield Row, San Diego, CA 92121, United States. Electronic address: vtanis@its.jnj.com.
