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51.
Willy Feller 《Mathematische Zeitschrift》1928,27(1):481-495
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Michael Bs Willy P. Burkard Jean-Luc Moreau Peter Schnholzer 《Helvetica chimica acta》1990,73(4):932-939
The synthesis of the title compound 2 and its diastereoisomer 3 was accomplished using tricarbonyl[1-5-n-(4-methoxycyclohexa-2,4-dien-1-yl)]iron tetrafluoroborate ( 4 ) as a precursor to the cyclohexanone ring. The assignments of the relative configurations of 2 and 3 are based on the X-ray analysis of compound 3 . Both compounds 2 and 3 are potent inhibitors of neuronal noradrenaline uptake in rats with similar potencies in vitro as compared to amitriptyline and desipramine. Compounds 2 and 3 are less potent as serotonin-uptake inhibitors, very weak inhibitors of dopamine uptake, and virtually devoid of antinociceptive activity. 相似文献
54.
Willy Gottschalk 《Fresenius' Journal of Analytical Chemistry》1908,47(4):237-240
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Willy Scherrer 《Commentarii Mathematici Helvetici》1929,1(1):69-119
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Willy Feller 《Mathematische Zeitschrift》1937,42(1):301-312
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Summary We characterize the ordinary generating functions of the Genocchi and median Genocchi numbers as unique solutions of some functional equations and give a direct algebraic proof of several continued fraction expansions for these functions. New relations between these numbers are also obtained. 相似文献
59.
Apyrimidinic/apurinic sites feature among the most prevalent DNA lesions. If not repaired, it has been recently evidenced that they are prone to react in situ with vicinal nucleobases, evolving toward more complex and highly mutagenic interstrand cross-links. Information concerning the structure and the multi-step reactivity leading to such clustered defects is scarce due to their low formation yield. This study reports a DFT exploration of the condensation reaction between a ketoaldehyde (derived from an oxidized C4’ abasic site) and three nucleobases featuring an amino group. They are found to present a very similar intrinsic reactivity, indicating in turn that differences of reactivity arise more from the relative positioning of the two reactive fragments within a flexible B-DNA. We also probe the role of a vicinal water molecule for the formation of the aminol and the requirements to reach an adequate estimate of this strongly exothermic reaction, which drives the DNA damage process. 相似文献
60.
Identification of Structure–Activity Relationships from Screening a Structurally Compact DNA‐Encoded Chemical Library
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Dr. Raphael M. Franzini Dr. Torun Ekblad Dr. Nan Zhong Moreno Wichert Willy Decurtins Angela Nauer Mauro Zimmermann Dr. Florent Samain Dr. Jörg Scheuermann Dr. Peter J. Brown Prof. Dr. Jonathan Hall Dr. Susanne Gräslund Prof. Dr. Herwig Schüler Prof. Dr. Dario Neri 《Angewandte Chemie (International ed. in English)》2015,54(13):3927-3931
Methods for the rapid and inexpensive discovery of hit compounds are essential for pharmaceutical research and DNA‐encoded chemical libraries represent promising tools for this purpose. We here report on the design and synthesis of DAL‐100K, a DNA‐encoded chemical library containing 103 200 structurally compact compounds. Affinity screening experiments and DNA‐sequencing analysis provided ligands with nanomolar affinities to several proteins, including prostate‐specific membrane antigen and tankyrase 1. Correlations of sequence counts with binding affinities and potencies of enzyme inhibition were observed and enabled the identification of structural features critical for activity. These results indicate that libraries of this type represent a useful source of small‐molecule binders for target proteins of pharmaceutical interest and information on structural features important for binding. 相似文献