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Novel pyrrolidine diketopiperazines selectively inhibit melanoma cells via induction of late-onset apoptosis.


ABSTRACT: A common liability of cancer drugs is toxicity to noncancerous cells. Thus, molecules are needed that are potent toward cancer cells while sparing healthy cells. The cost of traditional cell-based HTS is dictated by the library size, which is typically in the hundreds of thousands of individual compounds. Mixture-based combinatorial libraries offer a cost-effective alternative to single-compound libraries while eliminating the need for molecular target validation. Presently, lung cancer and melanoma cells were screened in parallel with healthy cells using a mixture-based library. A novel class of compounds was discovered that selectively inhibited melanoma cell growth via apoptosis with submicromolar potency while sparing healthy cells. Additionally, the cost of screening and biological fo

SUBMITTER: Onwuha-Ekpete L 

PROVIDER: S-EPMC3983399 | biostudies-literature | 2014 Feb

REPOSITORIES: biostudies-literature