Design, Synthesis and Structure-Activity Relationship Studies of Small Molecules Inhibiting Cancer Cell Growth
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Malignant melanoma is one of the most aggressive types of human cancers, and deregulation of C-MYC in late melanoma was observed. The fact that C-MYC depletion caused marked proliferation arrest indicated that C-MYC inhibition is highly possible to become a melanoma treatment. Dr. Mikhail Nikiforov from Roswell Park screened library containing 34,000 small molecule and discovered a compound, N77A7, capable of inhibiting growth of melanoma cell lines. It also showed promising melanoma-specificity and in vivo activity. N77A7 and 13 additional analogs were made for the structure-activity relationship study. Zinc chelation of N77A7 was also investigated as a possible mechanism of cancer cell growth inhibition.