Syntheses, biological evaluation and SAR of ingenol mebutate analogues for treatment of actinic keratosis and non-melanoma skin cancer
Ingenol mebutate is the active ingredient in Picato a new drug for the treatment of actinic keratosis. A number of derivatives related to ingenol mebutate were prepared by chemical synthesis from ingenol with the purpose of investigating the SAR and potency in assays relating to pro-inflammatory effects (induction of PMN oxidative burst and keratinocyte cytokine release), the potential of cell death induction, as well as the chemical stability. By modifications of the ingenol scaffold several prerequisites for activity were identified. The chemical stability of the compounds could be linked to an acyl migration mechanism. We were able to find analogues of ingenol mebutate with comparable in vitro properties. Some key features for potent and more stable ingenol derivatives have been identified.
On the Chemistry of Ingenol, II. Esters of Ingenol and δ7,8-Isoingenol
Preparation and purification of 3-acylated of ingenol (1a) structurally related to naturally occuring, irritant and cocarcinogenic principles are described.It is shown that 3-acylated partly rearrange to corresponding 5-acylates when they are chromatograp
Sorg, Bernd,Hecker, Erich
p. 748 - 756
(2007/10/02)
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