Synthesis, characterization and anticancer screening of some novel piperonyl–tetrazole derivatives

• Synthesis of new series of 1,2-substituted tetrazoles.
• The compounds were screened for ER+/− breast cancer cell lines.
• Three cell lines MCF-7, MDA-MB-231 and ZR-75 cells were used.
• HepG2 cells were used to find out the target specific character of compounds.
• The compounds with 10–30% retarding effects were screened unto gene level.

A series of new 1,2-substituted tetrazole derivatives were synthesized and evaluated on MCF-7 (ER positive), MDA-MB-231 and ZR-75 (ER negative) breast cancer cell lines. Out of the fourteen compounds, three compounds 10, 12 and 14 showed higher inhibitory effects on MCF-7 cells. Whereas, compound 8 exhibited higher inhibition in MDA-MB-231 and ZR-75 cells at 10−5 M concentration. Total RNA was extracted and effect of compounds on different marker genes was studied. The gene expression of CD44, BRAC and BAX were significantly affected. The compounds were screened against the HepG2 cell line, to know if they are selectively targeting specific cancers and only 1–10 percent inhibition was found at 10−5 M concentration.

1,2-Substitued tetrazole derivatives were synthesized and screened in ER positive and negative Breast cancer cell lines. Derivatives which showed 10–30 percent negative growth were studied unto marker gene expression.Figure optionsDownload as PowerPoint slide