The design and synthesis of a novel series of indole-analogues of indanocine is reported, together with their antiproliferative activity in the NCI's panel of cancer cell lines. Indanocine displays potent activity against a wide range of cancer cell lines (mean GI 50 < 20 nM), including drug-resistant cancer cell lines, and also inhibits the migration of metastatic cancer cells. A number of the described indole-analogues display a similar activity profile to indanocine, exhibiting potent antiproliferative activities in several cancer cell lines, and offer new leads for further development.
A high yielding three-component reaction between -iodo ethylamine derivatives, MeOH and gaseous CO 2 at ambient temperatures and pressures is reported using silver(I) oxide. Unfunctionalised alkyl iodides were also found to be effective in this transformation and their optimisation is also described. To highlight the ease and control at which gaseous CO 2 can be captured and functionalised under mild conditions, the reaction was performed using 13 C-enriched CO 2 to afford specifically 13 C-carbonyllabelled dialkyl carbonates with exquisite control of the isotopic purity in good yields and without the need for specialised equipment.
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