- Reversing Chemoselectivity: Simultaneous Positive and Negative Catalysis by Chemically Equivalent Rims of a Cucurbit[7]uril Host
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Enzyme catalysis has always been an inspiration and an unattainable goal for chemists due to features such as high specificity, selectivity, and efficiency. Here, we disclose a feature neither common in enzymes nor ever described for enzyme mimics, but one that could prove crucial for the catalytic performance of the latter, namely the ability to catalyze and inhibit two different reactions at the same time. Remarkably, this can be realized by two identical, spatially resolved catalytic sites. In the future, such a synchronized catalyst action could be used not only for controlling chemoselectivity, as in the present case, but also for regulating other types of chemical reactivity.
- Rad, Nazar,Danylyuk, Oksana,Sashuk, Volodymyr
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supporting information
p. 11340 - 11343
(2019/07/16)
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- Design, synthesis and biological evaluation of novel 4-anlinoquinazoline derivatives as EGFR inhibitors with the potential to inhibit the gefitinib-resistant nonsmall cell lung cancers
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A series of quinazoline derivatives with benzylidene hydrazine carboxamide were designed and synthesised as EGFR inhibitors. Most compounds exhibited exceptional anti-proliferative activity against A549, HepG2, MCF-7 and H1975 cells. Furthermore, six compounds demonstrated excellent inhibition activity against EGFRWT with the IC50 value both less than 2 nM. Among the six compounds, 44 exhibited the strongest activity (0.4 nM) and potently inhibited EGFRL858R/T790M (0.1 μM). Excitingly, the most potent compound 14 showed excellent enzyme inhibitory activity with 6.3 nM and 8.4 nM for both EGFRWT and EGFRT790M/L858R. The result of AO single staining and Annexin V/PI staining showed that the compound 14 and 44 could induce remarkable apoptosis of A549 cells. The compound 14 arrested the cell cycle at the S phase and compound 44 arrested the cell cycle at the G0 phase in A549 cells. These preliminary results demonstrate that compound 14 and 44 may be promising lead compound-targeting EGFR.
- Wang, Caolin,Xu, Shan,Peng, Liang,Zhang, Bingliang,Zhang, Hong,Hu, Yingying,Zheng, Pengwu,Zhu, Wufu
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p. 204 - 218
(2019/01/03)
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- Development of a water-soluble 3-formylBODIPY dye for fluorogenic sensing and cell imaging of sulfur dioxide derivatives
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A new water-soluble, highly fluorogenic 3-formylBODIPY dye that enables the sensing of SO2 derivatives in aqueous buffers and cancer cells is reported. The quaternary ammonium group appended through the meso-position of the BODIPY dye ensures water solubility. The probe exhibits high specificity for cytosolic (bi)sulfites and fluoresces brightly in human lung adenocarcinoma cells (A549).
- I??k, Murat,Simsek Turan, Ilke,Dartar, Suay
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supporting information
p. 1421 - 1425
(2019/04/30)
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- Effect of the Catalyst Nature on the Structure of Products of the Reaction of 4-(Dibromomethyl)Benzaldehyde with Trialkyl Orthoformates
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Reactions of 4-(dibromomethyl)benzaldehyde with trialkyl orthoformates in the presence of both Br?nsted (H2SO4) and Lewis (ZnCl2) acids involved acetalization of the aldehyde group. In the first case, the corresponding acetal is formed as the only product, whereas in the second case the reaction is accompanied by transformation of the dibromomethyl group to give terephthalaldehyde and its mono- and bis-acetals.
- Gazizov,Ivanova, S. Yu.,Bashkirtseva, N. Yu.,Ibragimov, Sh. N.,Khairullin,Gazizova,Kostenko
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p. 2783 - 2788
(2018/02/21)
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- Green synthesis and photophysical properties of novel 1H-imidazo[4,5-f][1,10]phenanthroline derivatives with blue/cyan two-photon excited fluorescence
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A simple, rapid, and highly efficient method has been developed for the synthesis of a series of novel 1H-imidazo[4,5-f][1,10]phenanthroline derivatives (1BN, 2Py, 3BI, 4BT, and 5MOBI) via a three–component, one–pot reaction under solvent–free conditions.
- Pan, Yu-Lu,Cai, Zhi-Bin,Bai, Li,Ma, Fei-Fei,Li, Sheng-Li,Tian, Yu-Peng
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p. 2886 - 2893
(2017/04/26)
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- METHODS OF USING DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY (ADP-RIBOSE)POLYMERASE (PARP)
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Provided herein are methods of treating cancer comprising administering a topoisomerase inhibitor, temozolomide, or a platin in combination with a Compound of Formula (I) or Formula (II), where the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein.
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Page/Page column 178
(2011/11/01)
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- DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP)
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A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.
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Page/Page column 91
(2010/03/02)
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- Synthesis of dipolar nitronyl nitroxides
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(equation presented) The synthesis of a nitronyl nitroxide radical with a dipolar (mesomeric betaine) unit is reported.
- Greve, Stefan,Naether, Christian,Friedrichsen, Willy
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p. 2269 - 2270
(2007/10/03)
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