- TARGETED RADIOPHARMACEUTICALS FOR THE DIAGNOSIS AND TREATMENT OF PROSTATE CANCER
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A compound of general formula (I): wherein: n is 1, 2 or 3; R1, R2, R3 and R4, independently represent OH or Q; and 20 Q represents a tissue-targeting moeity selected from the group consisting of or a stereoisomer, a hydrate, a solvate, or a salt thereof, or a mixture of same, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said 25 compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of soft tissue diseases, as a sole agent or in combination with other active ingredients.
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- Novel combretastatin analogues endowed with antitumor activity
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We studied the anticancer activity of a series of new combretastatin derivatives with B-ring modifications. The structure-activity relationship (SAR) information confirmed the importance of cis-stereochemistry and of a phenolic moiety in B-ring. We select
- Simoni, Daniele,Romagnoli, Romeo,Baruchello, Riccardo,Rondanin, Riccardo,Rizzi, Michele,Pavani, Maria Giovanna,Alloatti, Domenico,Giannini, Giuseppe,Marcellini, Marcella,Riccioni, Teresa,Castorina, Massimo,Guglielmi, Mario B.,Bucci, Federica,Carminati, Paolo,Pisano, Claudio
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p. 3143 - 3152
(2007/10/03)
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- COMBRETASTATIN DERIVATIVES WITH CYTOTOXIC ACTION
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The invention described herein relates to new combretastatin derivatives obtained by total synthesis and having the following general formula (I) in which the groups are as defined in the description here below. Said compounds, though chemically related to the structure of cis/trans-combretastatin, do not always bind tubulin, but nevertheless exhibit cytotoxic activity of interest in the oncological field as anticancer and/or antiangiogenic agents.
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- 2-Substituted-1-naphthols as potent 5-lipoxygenase inhibitors with topical antiinflammatory activity
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The synthesis, biological evaluation, and structure-activity relationships of a series of 1-naphthols bearing carbon substituents at the 2-position are described. These compounds are potent inhibitors of the 5-lipoxygenase from RBL-1 cells and also inhibi
- Batt,Maynard,Petraitis,Shaw,Galbraith,Harris
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p. 360 - 370
(2007/10/02)
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