Cytotoxic activity evolution of bichalcones through the piperazine Mannich Base linkage analogs on a panel of 25 human cancer cell lines

A series of novel bichalcone analogs through the piperazine Mannich base linkage, were synthesized (3-23) previously, using a Claisen-Schmidt Condensation reaction and structurally they are confirmed by spectral analysis including 1H, 13C NMR, IR and Mass analysis.These compounds were evaluated for their cytotoxic activity against using a panel of 25 human cancer cell lines including GBM-8401, MO59K, SH-SY5Y, NT-2, NPC 039, NPC 076, Fa Du, CE146T/VGH, HSC-3, CAL-27, SAS, A549, H-460, SK1-CP1, Huh-7, HepG2, Hep3B, MDA-MB-231, MCF7, A375, HeLa, MG-63, U-2 OS, HT-29 and Colo 25.Out of the 23 bichalcone analogs, compounds 3, 4 and 20 were showed more potent cytotoxic activity against tested all cancer cell lines.Compound 3 and 20 were exhibited more cytotoxic activity against tested all cancer cell lines with IC 50 values like GBM-8401 (IC 50 0.4 0.02 M), NPC039 (IC 50 0.6 0.04 M), NPC076 (IC 50 0.6 0.04 M), FaDu (IC 50 0.8 0.12 M), CE146/VGH (IC 50 1 0.06 M), HSC-3 (IC 50 1 0.06 M), CAL-27 (IC 50 0.4 0.04 M), A549 (IC 50 0.8 0.04 M), H460 (IC 50 0.6 0.06 M), SK1-CP1(IC 50 0.8 0.02 M), Hep G2 (IC50 0.6 0.02 M), MDA-MB-231 (IC50 0.8 0.04 M), MCF-7 (IC50 0.8 0.06 M), A375 (IC 50 0.6 0.06 M), HeLa (IC50 0.8 0.06 M), MG-63 (IC50 0.6 0.04 M), U-1 OS (IC50 0.6 0.02 M) and GBM-8401 (IC50 1.0 0.08 M), CE146T/VGH (IC50 6.0 0.05 M), CAL-27 (IC50 1.0 0.12 M), H460 (IC 50 10 M), SK1-CP1 (IC 50 2.0 0.12 M), MDA-MB-231 (IC 50 2.0 0.03 M), MCF-7 (IC 50 4.0 0.07 M), A375 (IC 50 0.8 0.02 M), HeLa (IC 50 2.0 0.04 M), MG-63 (IC 50 1.0 0.06 M), U-2OS (IC 50 1.0 0.08 M) and HT-29 (IC 50 4.0 0.08 M), respectively.Structure activity relationships of cytotoxicity are also discussed for active compounds on cancer cell lines.