The variety of structures and bonding modes of nitrogen-containing heterocyclic compounds make them potential therapeutic candidates for cancer, with lung cancer as an example. Novel epigenetic modulators were first monitored using a LDR (locus derepression) cell-based assay, and the results show different responses for 13 analogues of the drug JIB-04 toward target cancer cells. On assessment of cytotoxicity, these 13 epigenetic drugs display different inhibition efficiencies towards the non-small cell lung cancer HCC4017 in a physiological environment. In particular, EPH135 displays the most selective inhibition effect on the proliferation of the cancer cell line HCC4017, but almost no effect on its patient match-pair, the human bronchial epithelial cell HBEC30KT. The combination of a pyridine moiety and the molecule’s relatively small size are both highly amenable to intramolecular hydrogen bonding and are believed to contribute to EPH135’s potency and selectivity.

Identification of epigenetic drugs that possess lung anticancer activity from a series of 13 analogues of JIB-04

251st National Meeting (2016)

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