- COUMARIN-MODIFIED ANDROGENS FOR THE TREATMENT OF PROSTATE CANCER
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Provided are androstane and dihydrotestosterone compounds functionalized with carbocyclic groups or heterocyclic groups that may be saturated or unsaturated. The compounds may be used in methods of inhibiting cell growth of malignant cells and/or hyperplastic cells and/or treating individuals having diseases associated with malignant cell growth (e.g., cancer, such as, for example, prostate cancer) and/or hyperplastic cell growth and/or molecular imaging of malignant cells and/or hyperplastic cells and/or inducing degradation of a target protein. Also provided are compositions.
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Paragraph 0115
(2020/11/12)
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- A mild titanium-catalyzed synthesis of functionalized amino coumarins as fluorescence labels
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In contrast to Bronsted and other Lewis acids ClTi(OiPr)3 is especially suited to catalyze the formation of amino-substituted coumarins from aminophenols and functionalized β-oxo esters in a Pechmann condensation. This straightforward protocol allows the synthesis of fluorescence labels and false fluorescent neurotransmitters.
- Wirtz, Lisa,Kazmaier, Uli
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supporting information; experimental part
p. 7062 - 7065
(2012/01/05)
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- Orthogonally protected thiazole and isoxazole diamino acids: An efficient synthetic route
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An efficient strategy has been developed for the synthesis of heteroaromatic amino acids (HAAs). These methods generate mono-or orthogonally protected diamino acids from bamino acids (see scheme). Their synthetic reliability and biological potential was d
- Butler, Jeffrey D.,Coffman, Keith C.,Ziebart, Kristin T.,Toney, Michael D.,Kurth, Mark J.
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supporting information; experimental part
p. 9002 - 9005
(2010/12/19)
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- Intramolecular N-H, O-H, and S-H Insertion Reactions. Synthesis of Heterocycles from α-Diazo β-Keto Esters
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Several aspects of the Rh2(OAc)4-catalyzed intramolecular N-H, O-H, and S-H insertion reactions have been studied.Examination of the effect of ring size revealed that four-, five- and six-membered nitrogen heterocycles can be efficiently prepared from the corresponding α-diazo β-keto ester precursors (9a-c), whereas competing C-H insertion prevented formation of the seven-membered heterocycle.Variations in solvent, temperature, and catalyst concentration were found to play an important role in determining the product distribution in the cyclization of the 6-carbamoyl 2-diazo 3-keto ester 9c.The intramolecular X-H insertion reaction has also been successful in the synthesis of oxygen (39) and sulfur (49) heterocycles as well as a heterocycle containing two (N, O) heteroatoms (34).
- Moyer, Mikel P.,Feldman, Paul L.,Rapoport, Henry
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p. 5223 - 5230
(2007/10/02)
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