Background: The 3,4-diyne substituted isocoumarins have been designed, synthesized and
explored as potential anti-proliferative agents.
Method: Ultrasound assisted synthesis of these compounds was carried out by using a three-step
method involving (i) Pd/C-Cu catalyzed cross-coupling between the methyl 2-iodobenzoate and buta-
1,3-diynylbenzene followed by (ii) I2-mediated electrophilic cyclization of the resultant 2-(alk-1-
ynyl)benzoate ester and (iii) subsequent alkynylation of 4-iodo-3-(phenylethynyl)-isocoumarin under
Conclusion: The synthesized compounds showed promising growth inhibition when tested against
MDA-MB 231 and K562 cancer cell lines.
Keywords: Isocoumarin, Pd/C, coupling, ultrasound, cancer, K562, VEGF.
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