ingenol and Keratosis--Actinic

ingenol has been researched along with Keratosis--Actinic* in 1 studies

Other Studies

1 other study(ies) available for ingenol and Keratosis--Actinic

Article	Year
Syntheses, biological evaluation and SAR of ingenol mebutate analogues for treatment of actinic keratosis and non-melanoma skin cancer. Bioorganic & medicinal chemistry letters, 2013, Oct-15, Volume: 23, Issue:20 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. Topics: Antineoplastic Agents; Apoptosis; Cell Line; Diterpenes; Humans; Interleukin-8; Keratinocytes; Keratosis, Actinic; Leukocytes, Mononuclear; Melanoma; Oxidative Stress; Reactive Oxygen Species; Skin Neoplasms; Structure-Activity Relationship; Tumor Necrosis Factor-alpha	2013

Article

Year

Syntheses, biological evaluation and SAR of ingenol mebutate analogues for treatment of actinic keratosis and non-melanoma skin cancer.

Bioorganic & medicinal chemistry letters, 2013, Oct-15, Volume: 23, Issue:20

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.

Topics: Antineoplastic Agents; Apoptosis; Cell Line; Diterpenes; Humans; Interleukin-8; Keratinocytes; Keratosis, Actinic; Leukocytes, Mononuclear; Melanoma; Oxidative Stress; Reactive Oxygen Species; Skin Neoplasms; Structure-Activity Relationship; Tumor Necrosis Factor-alpha

2013