Since its initial isolation in 2009, bisebromoamide (BBA) has been identified as targeting the ERK and Akt pathways in renal cell carcinoma cell lines,7 and has been shown to be the first linear peptide to target actin.8 Through the generation of thiazoline analogues (Tz‐BBA) we have been able to pursue an SPPS‐based approach towards SAR investigations for the first time; four analogues (Bis1–4) showed nanomolar cytotoxic activity against the human colon tumour cell‐line HCT116. The gene discussed is AKT1; the disease is renal cell carcinoma.