Based on the fact that most commercially available TKIs are ATP-competitive inhibitors for binding at the catalytic domain of the EGFR tyrosine kinase (Traxler and Furet, 1999; Grünwald and Hidalgo, 2003; Normanno et al., 2003), we envisioned that replacement of the phenyl ring on the right side of WZ4002 with a chiral ribosyl moiety would provide compound 1 as a novel type of carbohydrate-based EGFR TKI against the drug resistance involved in NSCLC (Figure 2). The gene discussed is EGFR; the disease is non-small cell lung carcinoma.