The skeletal transformations of diterpenoid forskolin were achieved employing an oxidative rearrangement strategy. A library of 52 forskolin analogues, including 12 CTD compounds and 40 SAR compounds with unique scaffolds/ring systems, was produced during the course of this work. Compounds 2c and 10c exhibited inhibition of nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells, with IC50 values of 0.3µM and 4.1µM.