Quinolone-based IMPDH inhibitors: introduction of basic residues on ring D and SAR of the corresponding mono, di and benzofused analogues PMID: 12565969

ADC Targets in Oncology

2026-04-10

Quinolone-based IMPDH inhibitors: introduction of basic residues on ring D and SAR of the corresponding mono, di and benzofused analogues

Bioorg Med Chem Lett. 2003 Feb 10;13(3):547-51. doi: 10.1016/s0960-894x(02)00945-9.

T G Murali Dhar ¹ , Scott H Watterson , Ping Chen , Zhongqi Shen , Henry H Gu , Derek Norris , Marianne Carlsen , Kristin D Haslow , William J Pitts , Junqing Guo , John Chorba , Catherine A Fleener , Katherine A Rouleau , Robert Townsend , Diane Hollenbaugh , Edwin J Iwanowicz

Affiliations

Abstract

The synthesis and the structure-activity relationships (SAR) of analogues derived from the introduction of basic residues on ring D of quinolone-based inhibitors of IMPDH are described. This led to the identification of compound 27 as a potent inhibitor of IMPDH with significantly improved aqueous solubility over the lead compound 1.