Synthesis and cytotoxic activity of some 4,6-diaza-A,B-dihomo-steroid bilactams

• Some 4,6-diaza-A,B-dihomo-steroids were synthesized via two different synthetic route.
• The antiproliferative activity of synthesized compounds was assayed.
• Compounds 2 and 7b displayed a good cytotoxic activity.
• The cytotoxicity of compounds is different along with the structure of side chain.

Using cholesterol, stigmasterol and sitosterol as starting materials, some 4,6-diaza-A,B-dihomo-steroid bilactams were synthesized via two different synthetic routes by oxidation, reduction, oximation, Beckman rearrangement, etc. The cytotoxic activity of the synthesized compounds against SGC 7901 (human ventriculi carcinoma), Bel-7404 (human liver carcinoma), HeLa (human cervical carcinoma) and HT-29 (colonic carcinoma) cancer cells were investigated. The results showed that compounds 2 and 7b displayed a good cytotoxic activity to the SGC 7901, Bel 7404 and HeLa tumor cell lines with the IC50 values of 11.6, 16.4, 13.9 and 13.1, 21.8, 13.1 μmol/L, respectively. Their cytotoxic activity is almost same as cisplatin to these cells. The information obtained from the studies may be useful for the design of novel chemotherapeutic drugs.

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