Comprehensive Survey of Chemical Libraries for Drug Discovery and Chemical Biology: 2007

Synthesis of Amino-Benzothiaoxazepine-1,1-dioxides Utilizing a Microwave-Assisted, SNAr Protocol

“…1 One aspect of this effort is the development of efficient methods to access collections of heterocycles for high-throughput screening (HTS). In this regard, the synthesis of core scaffolds on multi-gram scale, followed by efficient parallel diversification is one approach to generate diverse compound collections for HTS.…”

One‐Pot Synthesis of New (1,3‐Thiazolo[5,4‐b]pyridin‐2‐yl)benzenediols and Their Antiproliferative Activities against Human Cancer Cell Lines

“…-The thiazole and fused-thiazole heterocycles are important structural components of biologically active molecules, and, as a result, they serve as attractive targets for developing new, effective synthesis methods [1] [2]. Because of their pharmaceutical importance in the area of drug discovery, we have been interested in developing an efficient protocol to prepare fused-thiazole scaffolds of 1,3-thiazolo [5,4-b]pyridine that is relatively unexplored with regard to its biological activity.…”

Triazole-Containing Isothiazolidine 1,1-Dioxide Library Synthesis: One-Pot, Multi-Component Protocols for Small Molecular Probe Discovery

“…This effort has been driven by the development and emergence of methods, protocols and technologies to access diverse collections of small molecules in a rapid fashion. 1 Sultams (cyclic sulfonamide analogues) have surfaced in recent years as important targets in drug discovery due to their extensive chemical and biological profiles. 2 In this regard, β-amino sultams and their corresponding sulfonate analogues are a relatively new chemotype that has shown interesting biological properties.…”