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A series of 1, 2, 3- triazole hybrids ( 9a - 9n ) were synthesised from major phenolic constituent, 4-methoxy ethyl cinnamate ( 5 ) isolated from rhizomes of  Hedychium spicatum  (Sm), a traditional medicinal plant used in variety of disease conditions. All the synthesised analogues were tested for their  in vitro  antiproliferative potential against HCT 116 (colon cancer), A549 (lung cancer), DU-145 (prostate cancer), Hep G2 (hepatoma) and HEK-293 (normal) cell lines. Among the compounds tested, compounds  9i  and  9k  potently arrested proliferation of DU-145 (prostate cancer) cell line. Compound  9i  displayed 20 times better antiproliferative potential than parent compound and almost identical inhibitory activity to that of the standard drug, doxorubicin. The flow cytometric analysis revealed that  9i  arrested cells in G2/M phase of cell cycle and induced apoptosis. Overall, the hybrid derivative  9i  was found to be a potential antiproliferative lead against prostate cancer.

natural product research

Synthesis and biological evaluation of 1,2,3-triazole hybrids of 4-methoxy ethyl cinnamate isolated from  Hedychium spicatum  (Sm) rhizomes: identification of antiproliferative lead actives against prostate cancer