- Fluorescent labeling of s2T-incorporated DNA and m5s2U-modified RNA
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We report herein comprehensive investigations of alkylation/sulfur exchange reactions of sulfur-containing substrates including nucleosides such as s2U, m5s2U, s4U, s2A and s2T-incorporated DNA enable by comprehensive screenings of the reagents (2a–2h). It has been proven that iodoacetamide (2a) displays the most promising feasibility toward sulfur-containing substrates including s2T, s2U, m5s2U, s4U and s2A. In sharp contrast, the alkylation process with S-benzyl methanethiosulfonate (BMTS, 2h) displays the best application potential only for s4U. Based on these results, the fluorescent labeling of s2T-incorporated DNA and m5s2U-modified RNA has been achieved. Supplemental data for this article is available online at https://doi.org/10.1080/15257770.2021.1942044.
- Yu, Ping,Zhou, Honglin,Li, Yuanyuan,Du, Zhifeng,Wang, Rui
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p. 754 - 766
(2021/07/06)
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- Natural Product Evodiamine with Borate Trigger Unit: Discovery of Potent Antitumor Agents against Colon Cancer
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In order to improve the antitumor potency of the natural product evodiamine, novel boron-containing evodiamine derivatives were designed by incorporating boronic acid and boronate as trigger units. Boronate derivative 13a could be triggered by reactive oxygen species (ROS) in the HCT116 colon cancer cell line and showed excellent antitumor activity in vitro and in vivo. It induced apoptosis in HCT116 cancer cells in a dose-dependent manner and cell growth arrest at the G2 phase.
- Li, Xinglin,Wu, Shanchao,Dong, Guoqiang,Chen, Shuqiang,Ma, Zonglin,Liu, Dan,Sheng, Chunquan
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p. 439 - 444
(2020/03/16)
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- Palladium-catalyzed carboxylative coupling of benzyl chlorides with allyltributylstannane: Remarkable effect of palladium nanoparticles
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Palladium-catalyzed carboxylative coupling of benzyl chlorides with allyltributylstannane was successfully conducted to produce benzyl but-3-enoates in satisfactory to good yields. The carboxylative coupling reaction occurred smoothly under mild conditions in the presence of palladium nanoparticles in tetrahydrofuran.
- Feng, Xiujuan,Sun, Anle,Zhang, Sheng,Yu, Xiaoqiang,Bao, Ming
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p. 108 - 111
(2013/04/10)
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- Regio- and chemoselective palladium-catalyzed benzylallylation of activated olefins: The remarkable effect of palladium nanoparticles
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The palladium-catalyzed three-component reactions of benzyl halides, activated olefins, and allyltributylstannane were successfully conducted to produce the corresponding benzylallylation products in satisfactory to high yields. The benzylallylation reaction proceeded smoothly under mild conditions in the presence of palladium nanoparticles in tetrahydrofuran. The Royal Society of Chemistry 2013.
- Zhang, Xuan,Feng, Xiujuan,Yu, Xiaoqiang,He, Ren,Bao, Ming
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p. 4016 - 4024
(2013/07/05)
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- A highly chemoselective and rapid chlorination of benzyl alcohols under neutral conditions
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A rapid and highly selective chlorination method has been developed using 2,4,6-trichloro-1,3,5-triazine (TCT) catalyzed by dimethyl sulfoxide. The reactions take 10 to 40 minutes, and the yields are almost quantitative. The neutral reaction conditions are compatible with substrates bearing acid-labile functional groups. Both competitive intramolecular and intermolecular reactions for benzyl alcohols in the presence of aliphatic alcohols indicate high selectivity. The procedure has been successfully used in the selective chlorination of gastrodin, a clinically used neuromedicine. This procedure represents a useful new tool in organic and medicinal chemistry. Georg Thieme Verlag Stuttgart.
- Sun, Lili,Peng, Guisheng,Niu, Hongmei,Wang, Qiang,Li, Chunbao
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experimental part
p. 3919 - 3924
(2009/05/26)
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- Chemical insights in the concept of hybrid drugs: The antitumor effect of nitric oxide-donating aspirin involves a quinone methide but not nitric oxide nor aspirin
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Hybrid drug 1 (NO-ASA) continues to attract intense research from chemists and biologists alike. It consists of ASA and a -ONO2 group connected through a spacer and is in preclinical development as an antitumor drug. We report that, contrary to current beliefs, neither ASA nor NO contributes to this antitumor effect. Rather, an unsubstituted QM was identified as the sole cytotoxic agent. QM forms from 1 after carboxylic ester hydrolysis and, in accordance with the HSAB theory, selectively reacts with cellular GSH, which in turn triggers cell death. Remarkably, a derivative lacking ASA and the -ONO 2 group is 10 times more effective than 1. Thus, our data provide a conclusive molecular mechanism for the antitumor activity of 1. Equally importantly, we show for the first time that a "presumed invisible" linker in a hybrid drug is not so invisible after all and is in fact solely responsible for the biological effect.
- Hulsman, Niels,Medema, Jan Paul,Bos, Carina,Jongejan, Aldo,Leurs, Rob,Smit, Martine J.,De Esch, Iwan J. P.,Richel, Dick,Wijtmans, Maikel
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p. 2424 - 2431
(2008/02/03)
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- Thiadiazole derivatives for the treatment of depressive states
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Thiadiazole derivatives of general formula (I) wherein R1 is selected from the class consisting of: C1-C10 linear or branched alkyl, benzyl, optionally substituted at the aromatic ring with one or more groups se
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- Process for the preparation of α-halogenated cresol esters
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Process for the preparation of Compound I by treating Compound II with X2 or SO2 X2 in the presence of a free radical initiator and an anhydride having the formula (RCO)2 O while eliminating the acid halide form
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- Quinone methide photograhpic reagent precursors
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Novel compounds are disclosed which release a photographic reagent in the presence of alkali and are therefore useful in photographic products and processes. The compounds may be defined as quinone- or naphthoquinonemethide precursors containing a mercapt
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