Background: Compounds containing furo[3,2-b]pyridine framework have shown interesting pharmacological
properties, including anticancer activities. Though these compounds are generally synthesized via the
heteroannulation processes involving acetylenic derivatives, some of them are complex.
Objective: The study aimed to explore a series of 2-substituted furo[3,2-b]pyridines for their cytotoxic properties
against cancer cell lines in vitro.
Methods: We developed a convenient synthesis of 2-substituted furo[3,2-b]pyridines via sequential (i) C-C
coupling followed by (ii) C-O bond-forming reactions in a single pot. The reactions were performed under ultrasound
irradiation in the presence of Pd/C as an inexpensive, stable and widely used catalyst. A range of 2-
substituted furo[3,2-b]pyridines were synthesized via coupling of 3-chloro-2-hydroxy pyridine with terminal
alkynes in the presence of 10% Pd/C-CuI-PPh3-Et3N in EtOH. The in vitro evaluation of all these compounds
was carried out against MDA-MB-231 and MCF-7 cell lines and subsequently against SIRT1.
Results: The furo[3,2-b]pyridine derivative 3b showed encouraging growth inhibition of both MDAMB-231
and MCF-7 cell lines and inhibition of SIRT1. The compound 3b also showed apoptosis-inducing potential
when tested against MCF-7 cells.
Conclusion: The Pd/C-Cu catalysis under ultrasound accomplished a one-pot and direct access to 2-substituted
furo[3,2-b]pyridine derivatives, some of which showed anticancer properties.