Modulators of HEC1 activity and methods therefor

摘要

Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Especially preferred compounds disrupt Nek2/Hec1 binding and are therefore useful as chemotherapeutic agent for neoplastic diseases.

主权项

1. A method of treating a neoplastic disease, comprising:
administering to a mammal in need thereof a pharmaceutical composition comprising a compound having a structure according to Formula I R1 is alkyl, ORa, SRa, or —S(O)2Ra; Ra is alkyl, or aryl substituted with alkoxy; R2 and R3 are independently alkyl; R4 is hydrogen; R5 is pyridyl optionally substituted with alkyl, fluoroalkyl, halogen, or alkoxy; wherein the compound is present in the composition an amount effective to disrupt Hec1/Nek2 binding in the mammal when the composition is administered to the mannal; and wherein the neoplastic disease is selected from the group consisting of breast cancer, prostate cancer, cervical cancer and leukemia.