Abstract

AbstractA series of coumarin tetrahydro‐β‐carboline hybrids 3 have been synthesized by the Pictet‐Spengler reaction. Stoichiometrically controlled DDQ oxidation has led to dihydro 4 and β‐carboline 5. In vitro anticancer activity against 60 cell lines has revealed the potency of 3 f, 4 a and 5 c. In silico studies indicate the binding properties of 5 c with Kinesin spindle protein (KSP) and tubulin protein. Gel electrophoresis studies revealed that compound 3 f partially cleaved the CT‐DNA, whereas the ring C aromatized compound 5 c completely cleaved the CT‐DNA. Structures of the newly synthesized compounds are confirmed by spectroscopic and X‐ray studies.

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