116606-76-9Relevant academic research and scientific papers
Synthesis and biological evaluation of new podophyllic aldehyde derivatives with cytotoxic and apoptosis-inducing activities
Castro, Ma. ángeles,Miguel Del Corral, José Ma.,García, Pablo A.,Rojo, Ma. Victoria,De La Iglesia-Vicente, Janis,Mollinedo, Faustino,Cuevas, Carmen,San Feliciano, Arturo
experimental part, p. 983 - 993 (2010/07/16)
Several series of nonlactonic podophyllic aldehyde analogues were prepared and evaluated against several human tumor cell lines. They had different combinations of aldehyde, imine, amine, ester, and amide functions at C-9 and C-9′ of the cyclolignan skeleton. All the compounds synthesized showed cytotoxicity levels in the μM range and below. Within the new series tested, compounds having an aldehyde or imine at C-9 and an ester at C-9′ were the most potent, with GI50 values in the nM range, some of them being several times more potent against HT-29 and A-549 carcinoma than against MB-231 melanoma cells. Cell cycle studies and analysis of the microtubule-disrupting capacity have demonstrated the existence of two different mechanisms of cell death induction for compounds with closely related structures.
