The structure-activity relations among herbimycins (herbimycin A (I), herbimycin B, and 19 derivatives of herbimycin A) were investigated with respect to the following activities: (1) reversing transformed cell morphol. to the normal one in ts/NRK cells at a permissive temperature (33°) and (2) inhibiting cell growth and macromol. syntheses under the same conditions.Furthermore, whether the transformation reversing activity of herbimycins was due to inhibition of src oncogene functions was also investigated.The results are discussed in comparison to their effects on Ehrlich ascites carcinoma in mice.