Design, Synthesis, and Biological Evaluation of Novel 1,3-Oxazole Sulfonamides as Tubulin Polymerization Inhibitors.

A series of novel 1,3-oxazole sulfonamides were constructed and screened for their potential to inhibit cancer cell growth. These compounds were evaluated against the full NCI-60 human tumor cell lines, with the majority exhibiting promising overall growth inhibitory properties. They displayed high specificity within the panel of leukemia cell lines versus all other lines tested.

Generation and reactivity of aza-oxyallyl cationic intermediates: aza-[4 + 3] cycloaddition reactions for heterocycle synthesis.

Aza-[4 + 3] cycloadditions of putative aza-oxyallyl cationic intermediates and cyclic dienes are reported. The intermediate is generated by the dehydrohalogenation of α-haloamides. The reaction is general to a variety of α-haloamides and is diastereoselective.