Synthesis and characterization of Sant-75 derivatives as Hedgehog-pathway inhibitors

Abstract

SummarySant-75 is a newly identified potent inhibitor of the hedgehog pathway. We designed a diversity-oriented synthesis program, and synthesized a series of Sant-75 analogues, which lays the foundation for further investigation of the structure–activity relationship of this important class of hedgehog-pathway inhibitors.

Self-Assembly of a Pd4Cu8L8 Cage for Epoxidation of Styrene and Its Derivatives

“…The subcomponent molecule 1-(pyridin-4-yl)-1H-imidazole-4-carbaldehyde (denoted as PIMC) was synthesized by copper­(I) catalyzed Ullmann condensation reaction of 4-bromopyridine and 1H-Imidazole-4-carboxaldehyde in dried dimethylformamide (DMF) (for details, see the Supporting Information), which was synthesized by following a modified procedure . The metalloligand CuL was obtained by heating the mixture of PIMC, 1,3-propylenediamine, and Cu­(NO 3 ) 2 ·3H 2 O in CH 3 CN at 60 °C (for details, see the Supporting Information) with a high yield (95%).…”

“…32−39 dimethylformamide (DMF) (for details, see the Supporting Information), which was synthesized by following a modified procedure. 40 The metalloligand CuL was obtained by heating the mixture of PIMC, 1,3-propylenediamine, and Cu(NO 3 ) 2 • 3H 2 O in CH 3 CN at 60 °C (for details, see the Supporting Information) with a high yield (95%). Then, the metalloligand CuL and Pd(NO 3 ) 2 •2H 2 O were dissolved in dimethyl sulfoxide (DMSO) and heated to 60 °C for 8 h to obtain cage 1.…”

One-Pot Syntheses of Isoquinolin-3-ones and Benzo-1,4-diazepin-2,5-diones Utilizing Ugi-4CR Post-Transformation Strategy

“…For many years our laboratories have been involved in developing a chemical genetic approach to analyze biological systems by way of interfacing libraries of small molecules with creative biological assays . As part of this research objective, we became interested in establishing a novel synthetic strategy to construct diverse isoquinolinone and benzodiazepine-based heterocycles.…”