- Characterization of a brain permeant fluorescent molecule and visualization of Aβ parenchymal plaques, using real-time multiphoton imaging in transgenic mice
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Emerging paradigms mandate discovery of imaging agents for diagnosing Alzheimer's disease (AD) prior to appearance of clinical symptoms. To accomplish this objective, a novel heterocyclic molecule (4) was synthesized and validated as Aβ targeted probe. The agent shows labeling of numerous diffuse Aβ plaques in confirmed AD human brain tissues and traverses the blood-brain barrier to enable labeling of parenchymal Aβ plaques in live mice (APP ±/PS1±) brains.
- Sundaram,Garai, Kanchan,Rath, Nigam P.,Yan, Ping,Cirrito, John R.,Cairns, Nigel J.,Lee, Jin-Moo,Sharma, Vijay
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Read Online
- Di- tert-butyl Peroxide-Mediated Radical C(sp2/sp3)-S Bond Cleavage and Group-Transfer Cyclization
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A novel strategy of cascade radical C(sp2/sp3)-S bond cleavage and group-transfer cyclization is disclosed. Triggered by alkyl radicals, varieties of 2-isocyanoaryl thioethers containing aliphatic, aryl, and heteroaromatic groups can be cleaved and precisely reinstalled to give benzothiazole derivatives. Mechanistic studies reveal that the cascade reaction undertakes an intermolecular pathway, and the inner radical sources (R radicals) exhibit high priority over those of methyl radical origin from di-tert-butyl peroxide.
- Luo, Kai,Yang, Wen-Chao,Wei, Kai,Liu, Yue,Wang, Jun-Ke,Wu, Lei
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supporting information
p. 7851 - 7856
(2019/10/11)
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- Rational design and synthesis of 2-anilinopyridinyl-benzothiazole Schiff bases as antimitotic agents
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Based on our previous results and literature precedence, a series of 2-anilinopyridinyl-benzothiazole Schiff bases were rationally designed by performing molecular modeling experiments on some selected molecules. The binding energies of the docked molecules were better than the E7010, and the Schiff base with trimethoxy group on benzothiazole moiety, 4y was the best. This was followed by the synthesis of a series of the designed molecules by a convenient synthetic route and evaluation of their anticancer potential. Most of the compounds have shown significant growth inhibition against the tested cell lines and the compound 4y exhibited good antiproliferative activity with a GI50 value of 3.8?μM specifically against the cell line DU145. In agreement with the docking results, 4y exerted cytotoxicity by the disruption of the microtubule dynamics by inhibiting tubulin polymerization via effective binding into colchicine domain, comparable to E7010. Detailed binding modes of 4y with colchicine binding site of tubulin were studied by molecular docking. Furthermore, 4y induced apoptosis as evidenced by biological studies like mitochondrial membrane potential, caspase-3, and Annexin V-FITC assays.
- Shaik, Thokhir B.,Hussaini, S.M. Ali,Nayak, V. Lakshma,Sucharitha, M. Lakshmi,Malik, M. Shaheer,Kamal, Ahmed
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supporting information
p. 2549 - 2558
(2017/05/09)
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- TRI-HETEROCYCLIC DERIVATIVES, PREPARATION PROCESS AND USES THEREOF
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The present invention relates to a tri-heterocyclic derivatives, preparation process and uses thereof, specifically relates to a tri-heterocyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, preparation process, and further relates to a pharmaceutically acceptable composition comprising compounds of formula (I), or a pharmaceutically acceptable salt thereof, and their pharmaceutical use as inhibitors of kinase.
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Paragraph 0121; 0223; 0224
(2014/11/13)
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- TRI-HETEROCYCLIC DERIVATIVES, PREPARATION PROCESS AND USES THEREOF
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The present invention relates to a tri-heterocyclic derivatives, preparation process and uses thereof, specifically relates to a tri-heterocyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, preparation process, and further relates to a pharmaceutically acceptable composition comprising compounds of formula (I), or a pharmaceutically acceptable salt thereof, and their pharmaceutical use as inhibitors of kinase
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Page/Page column 28; 29
(2013/07/05)
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- Searching for new cures for tuberculosis: Design, synthesis, and biological evaluation of 2-methylbenzothiazoles
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The actual development and clinical use of new therapeutics for tuberculosis (TB) have remained stagnant for years because of the complexity of the disease process, the treatment of which at present requires the administration of drug combinations over a 6month period. There is thus an urgent need for the discovery and development of novel, more active, and less toxic anti-TB agents. In this study, we report on the chemistry and biology of a series of potent 5-(2-methylbenzothiazol-5-yloxymethyl) isoxazole-3-carboxamide derivatives, which proved to be active against replicating Mycobacterium tuberculosis (Mtb) H37Rv. The most potent compounds 7j and 7s were found to inhibit Mtb growth at micromolar concentrations, with MICvalues of 1.4 and 1.9 μM, respectively. Impressively, all active compounds were nontoxic toward Vero cells (IC50 > 128 μM). Moreover, the best of these compounds were also tested against protozoan parasites, and some of these compounds were found to show activity, especially against Plasmodium falciparum. These studies thus suggest that certain 2-methylbenzothiazole based compounds may serve as promising lead scaffolds for further elaboration as anti-TB drugs and as possible antimalaria drugs. 2009 American Chemical Society.
- Huang, Qingqing,Mao, Jialin,Wan, Baojie,Wang, Yuehong,Brun, Reto,Franzblau, Scott G.,Kozikowski, Alan P.
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supporting information; experimental part
p. 6757 - 6767
(2010/04/24)
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- Benzazole compounds and their use
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The present invention discloses a method for repelling insects, mites and ticks from warm-blooded animals with a benzazole compound.
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