Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Compounds of the invention disrupt Hec1/Nek2 interaction, and may therefore be useful as chemotherapeutic agents for neoplastic disease.本發明提供調節Hec1/Nek2之交互作用的各種化合物、組合物及方法,其中,本發明之合物可阻斷Hec1/Nek2之交互作用因此可以適用於腫瘤性疾病之化療藥劑。