A variety of functionalities were introduced at 2-aroylquinoline’s C5 position, which is considered equivalent to C-3′ of the B-ring of CA4, via Suzuki arylation, Sonogashira ethynylation, and Rosenmund–von Braun cyanation. These substitutions are rarely utilized in the modification of 3′-OH of CA4. The resulting products 6 and 7 having cyano and ethynyl groups exhibited comparable antiproliferative and tubulin inhibitory activities to colchicine.
Organic & Biomolecular Chemistry
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