Starting materials were purchased from Sigma-Aldrich or Fisher Scientific. ACS grade methanol, ethyl acetate, toluene, anhydrous DMF, NMP, and DMSO were purchased from Fisher Scientific or Sigma-Aldrich. ITZ analogue 9 was purchased from Toronto Research Chemicals. All reactions were run under an argon atmosphere. NMR data was collected on a Bruker AVANCE 500 MHz spectrometer and analysis performed using MestReNova. HRMS data was analyzed at the Mass Spectrometry Facility at the University of Connecticut by Dr. You-Jun Fu. FT-IR analysis was performed on a Bruker Alpha Platinum ATR instrument using OPUS software (v 7.2). The preparation of previously characterized ITZ intermediates followed known procedures with minor modifications.24 (link)-26 (link),32 (link) X-ray crystals were prepared using vapor diffusion techniques (pentanes:chloroform) and analysis performed by Dr. Victor Day at the Small-Molecule X-ray Crystallography Lab at the University of Kansas on a Bruker MicroStar microfocus Cu rotating anode generator with two CCD detectors or a Bruker Apex II CCD detector equipped with Helios multilayer optics instruments. Mercury (v3.0) software was used to visualize X-ray structural analysis. All ITZ analogues evaluated in the biological assays (1-25) were greater than 95% pure based on the HPLC methods described below.