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Five new 4-aza-2,3-didehydropodophyllotoxins were synthesized by a straightforward multi-component reaction in the hope of finding new structures with interesting anticancer activity. The "one-pot" synthesis process is developed to increase performance as well as minimize the steps involved. The obtained compounds with podophyllotoxin frame have the corresponding yields of 60-83%. Five new 4-aza-2,3-didehydropodophyllotoxins demonstrated comparable cytotoxicity against the Hep-G2, MCF7celldoi:10.15625/2525-2518/15577 fatcat:jclzwkvuhnem3phlyymwuaxwrm