Follow‐up structure‐guided chemistry resulted in synthesizing MIV‐6R with IC50 (Kdisp) value of 56 nM that inhibited proliferation and induced hematopoietic differentiation in MLL1‐AF9, ‐AF6, and ‐AF1p fusion leukemia cells indicating behaviour independent of the fusion partner.112 Orally bioavailable derivatives of MI‐2‐2, MI‐503, and MI‐463 were developed that inhibited the growth of MLL1 fusion cell lines, induced differentiation and were effective in the xenograft models blocking leukemia progression.113. The gene discussed is MLLT3; the disease is leukemia.