| 1. |
- Dahlén, Kristian, 1973, et al.
(författare)
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A scaffold approach to 3,6,8-trisubstituted flavones
- 2006
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Ingår i: Synlett. - : Georg Thieme Verlag KG. - 0936-5214 .- 1437-2096. ; :6, s. 897-900
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Tidskriftsartikel (refereegranskat)abstract
- An efficient synthetic approach to 3,6,8-trisubstituted flavone scaffolds has been developed based on Pd-mediated coupling reactions.
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| 2. |
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| 3. |
- Dahlén, Kristian, 1973, et al.
(författare)
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Synthesis of 2,3,6,8-tetrasubstituted chromone scaffolds.
- 2006
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Ingår i: The Journal of organic chemistry. - : American Chemical Society (ACS). - 0022-3263 .- 1520-6904. ; 71:18, s. 6863-6871
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Tidskriftsartikel (refereegranskat)abstract
- A useful and efficient synthetic strategy to 2,3,6,8-tetrasubstituted chromone derivatives has been developed. 2-Aryl/styryl-8-bromo-6-chloro-3-hydroxychromone derivatives were synthesized and used as scaffolds by introducing a variety of substituents in the 3-, 6-, and 8-positions using palladium-mediated reactions. Excellent regioselectivity in all positions could be obtained by performing reactions in the 8-position first, in which Stille, Heck, Suzuki, and Sonogashira reactions gave good to excellent yields of product (63-98%). Stille and Heck reactions in the 6-position also gave the desired products in good yields (64-86%). The hydroxy group in the 3-position was activated as a triflate and used in productive Stille reactions (63-94%). This hydroxyl group was also used in O-alkylation reactions with different functionalized alkyl bromides (57-88%). The flavonoids, which are based on the chromone structure, and other related ring systems, have several interesting biological activities. The chromones are also interesting structural scaffolds, and they have for example been designed to be used as mimetics of short peptides. The versatile applicability of chromone derivatives and especially their potential use in drug discovery implicates the importance of access to efficient synthetic routes to such compounds.
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| 4. |
- Dyrager, Christine, 1975, et al.
(författare)
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2,6,8-Trisubstituted 3-hydroxychromone derivatives as fluorophores for live-cell imaging.
- 2009
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Ingår i: Chemistry (Weinheim an der Bergstrasse, Germany). - : Wiley. - 1521-3765 .- 0947-6539. ; 15:37, s. 9417-23
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Tidskriftsartikel (refereegranskat)abstract
- We present the synthesis and photophysical characterisation of a series of structurally diverse, fluorescent 2,6,8-trisubstituted 3-hydroxychromone derivatives with high fluorescence quantum yields and molar extinction coefficients. Two of these derivatives (9 and 10 a) have been studied as fluorophores for cellular imaging in HeLa cells and show excellent permeability and promising fluorescence properties in a cellular environment. In addition, we have demonstrated by photophysical characterisation of 3-isobutyroxychromone derivatives that esterification of the 3-hydroxyl group results in acceptable and useful fluorescence properties.
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| 5. |
- Dyrager, Christine, 1975, et al.
(författare)
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Inhibitors and promoters of tubulin polymerization : Synthesis and biological evaluation of chalcones and related dienones as potential anticancer agents
- 2011
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Ingår i: Bioorganic & Medicinal Chemistry. - : Elsevier BV. - 0968-0896 .- 1464-3391. ; 19:8, s. 2659-2665
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Tidskriftsartikel (refereegranskat)abstract
- A series of dihalogenated chalcones and structurally related dienones were synthesized and evaluated for their antiproliferative activity in 10 different cancer cell lines and for their effect on microtubule assembly. All compounds showed cytotoxic activity, with IC50 values in the 5-280 mu M range depending on the chalcone structure and the cell line. Five of the compounds were found to be tubulin polymerization inhibitors. In contrast, one of the compounds was found to stabilize tubulin to the same extent as the anticancer drug docetaxel. Molecular modeling suggested that the tubulin inhibitors bind to the colchicine binding site of beta-tubulin while the novel tubulin stabilization agent seems to interact with the paclitaxel binding site.
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| 6. |
- Fridén-Saxin, Maria, 1979, et al.
(författare)
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Chroman-4-one and chromone based somatostatin beta-turn mimetics
- 2016
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Ingår i: European Journal of Medicinal Chemistry. - : Elsevier BV. - 0223-5234. ; 114, s. 59-64
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Tidskriftsartikel (refereegranskat)abstract
- A scaffold approach has been used to develop somatostatin beta-turn mimetics based on chroman-4-one and chromone ring systems. Such derivatives could adopt conformations resembling type II or type II' beta-turns. Side chain equivalents of the crucial Trp8 and Lys9 in somatostatin were introduced in the 2- and 8-positions of the scaffolds using efficient reactions. Interestingly, this proof-of-concept study shows that 4 and 9 have K-i-values in the low mu M range when evaluated for their affinity for the sst2 and sst4 receptors. (C) 2016 Elsevier Masson SAS. All rights reserved.
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| 7. |
- Moraru, Ruxandra, et al.
(författare)
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Evaluation of oral health knowledge among personnel in an institution for the rehabilitation of disabled young adults
- 2007
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Ingår i: Journal of Disability and Oral Health. ; 8:3, s. 135-141
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Tidskriftsartikel (refereegranskat)abstract
- Aim and objectives: To explore the views and knowledge on oral health care by caregivers working in the Bucharest residential centre, Recuperation and Rehabilitee Centre for Persons with Handicap, using a questionnaire. Design: The questionnaire was translated from Swedish into Romanian and consisted of 30 questions; 18 were closed questions with three to four alternatives, 12 were constructed as a Visual Analogue Scale (VAS). The questionnaire was devised to generate information in three broad areas; personal data, extent of knowledge and current practices. The questionnaire was distributed to 164 staff members by a physician and a co-author (MG). The questionnaire was answered anonymously. Results: Of the 164 employees of the CRRPH, 70 answered the questionnaire. The results showed a lack of knowledge concerning oral health and factors influencing oral diseases. Knowledge of the oral health of the patients at the residential centre was limited. Further, the staff efforts to help the patients were overly optimistic. Conclusions: The results indicate a gap between knowledge and practice in caregivers toward the oral health care of multiply impaired residents. The study concludes that improvements in oral health can be encouraged by working with staff knowledge, attitudes, values and beliefs.
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| 8. |
- Wallén, Erik A A, et al.
(författare)
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Synthesis of 3-aminomethyl-2-aryl- 8-bromo-6-chlorochromones.
- 2007
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Ingår i: Organic letters. - : American Chemical Society (ACS). - 1523-7060 .- 1523-7052. ; 9:3, s. 389-91
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Tidskriftsartikel (refereegranskat)abstract
- [reaction: see text] An efficient synthetic route to Cbz-protected 3-aminomethyl-2-aryl-8-bromo-6-chlorochromones has been developed. 3-Aryl-1-(3-bromo-5-chloro-2-hydroxyphenyl)-2-propen-1-one or 2-aryl-8-bromo-6-chlorochroman-4-one could be reacted under Mannich conditions yielding 2-aryl-8-bromo-6-chloro-3-methylenechroman-4-one, which was further converted to the target compound via an aza-Michael reaction followed by an SeO(2) oxidation. This procedure represents a new method to introduce a primary aminomethyl group at the 3-position of a 2-arylchromone scaffold. The Cbz-protected 3-aminomethyl-2-aryl-8-bromo-6-chlorochromones can, e.g., be used in the synthesis of chromone-based beta-turn peptidomimetics.
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