The aim of this study was to investigate the effect of pentacyclic triterpenoids-reduced Lantadenes A (3) and B (4) on the cytotoxicity, stimulation of apoptosis and regulation of transcription factors in HL-60 cells. The 3 and 4 are the minor compounds of weed Lantana camara L. (Verbenaceae) and were prepared semi-synthetically in single step by reducing Lantadenes A (1) and B (2) under microwave irradiation with yield of 98–99 %. The 3 and 4 demonstrated selective cytotoxicity against HL-60, MCF-7, HSC-2, and HCT-116 cancer cell lines (IC50 1.2–6.4 lM) and were found non-toxic toward normal cells (VERO) with IC50[50). The compounds 3 and 4 (15 lM)-induced apoptosis by activation of caspase-3 and bax, along with significant decrease in expression of NF-rB (p-65) and bcl-2 in HL-60 cells. The compounds 3 and 4 at 15 lM significantly suppressed the production of nitrite, TNF-a, and iNOS gene expression in HL-60 cells. The results suggested that reduced Lantadenes A and B have the potential to be developed as anticancer agents.