42174-73-2Relevant articles and documents
S,O-Ligand-Promoted Pd-Catalyzed C?H Olefination of Anisole Derivatives
Fernández-Ibá?ez, M. ángeles,Jia, Wen-Liang,Sukowski, Verena,van Borselen, Manuela,van Diest, Rianne
supporting information, p. 4132 - 4135 (2021/08/24)
The C?H olefination of substituted anisole derivatives by a Pd/S,O-ligand catalyst is reported. The reaction proceeds under mild conditions with a broad range of substituted aryl ethers bearing both electron donating and withdrawing substituents at ortho,
Synthesis of methoxylated goniothalamin, aza-goniothalamin and γ-pyrones and their in vitro evaluation against human cancer cells
Barcelos, Rosimeire Coura,Pastre, Julio Cezar,Caixeta, Vanessa,Vendramini-Costa, Débora Barbosa,De Carvalho, Jo?o Ernesto,Pilli, Ronaldo Aloise
experimental part, p. 3635 - 3651 (2012/07/27)
The present work describes the preparation of three novel series of compounds based on the structure of goniothalamin, a natural styryl lactone which has been found to display cytotoxic and antiproliferative activities against a variety of cancer cell lines. A focused library of 29 novel goniothalamin analogues was prepared and evaluated against seven human cancer cell lines. While the γ-pyrones and the aza-goniothalamin analogues were less potent than the lead compound, 2,4-dimethoxy analogue 88 has shown to be more potent in vitro than goniothalamin against all cancer cell lines evaluated. Furthermore, it was more potent than doxorubicin against NCI-ADR/RES, OVCAR-03 and HT-29 while being less toxic to human keratinocytes (HaCat). The 3,5-dimethoxy analogue 90 and 2,4,5-trimethoxy analogue 92 also displayed promising antiproliferative activity when compared to goniothalamin (1). These results provide new elements for the design and synthesis of novel representatives of this family of natural compounds.
Acid-labile anchor groups for the synthesis of peptide amides by a solid-phase method
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, (2008/06/13)
The invention relates to new compounds of the formula STR1 in which R1 denotes (C1 -C8)-alkyl, R2 denotes an amino acid residue which is protected with a urethane protective group which can be eliminated with weak acid or base, or denotes an amino protective group which can be eliminated with weak acid or base, R3 denotes hydrogen or (C1 -C4)-alkyl, and Y1 -Y9 denote identical or different radicals hydrogen, (C1 -C4)-alkyl, (C1 -C4)-alkoxy or --O--(CH2)n --COOH (with n=1 to 6), with one of these radicals being --O--(CH2)n --COOH, or Y1, Y2 and Y5 -Y9 denote identical or different radicals hydrogen, (C1 -C4)-alkyl or (C1 -C4)-alkoxy, Y3 denotes hydrogen or (C1 -C8)-alkoxy and Y4 denotes --(CH2)n --COOH or --NH--CO--(CH2)n --COOH (with n=1 to 6). Processes for the preparation thereof and the synthesis of peptide amides by a solid-phase method using these new compounds (spacers) are described.