- A novel near-infrared chemosensor for mercury ion detection based on D-A structure of triphenylamine and benzothiadiazole
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A novel near infrared ratiometric fluorescent chemosensor based on triphenylamine, thiophene and benzothiadiazole has been developed. The emission wavelength of sensor DTPAT-BT-S was in the near infrared region. The wavelength changed from 656?nm to 723?n
- Zhang, Qisong,Zhang, Jian,Zuo, Hujin,Wang, Chengyun,Shen, Yongjia
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- A novel colorimetric and fluorescent sensor for cyanide anions detection based on triphenylamine and benzothiadiazole
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A chemical sensor containing triphenylamine and benzothiadiazole for cyanide anions detection was designed and synthesized, whose structural feature is a donor-acceptor-donor (D-A-D) molecular configuration, which is substituted with a dicyanovinyl group
- Zhang, Qisong,Zhang, Jian,Zuo, Hujin,Wang, Chengyun,Shen, Yongjia
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- Piperidine compound and preparation method and medical application thereof
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The invention discloses a piperidine compound shown as a formula (I) and a preparation method and medical application thereof, and particularly relates to a piperidine USP7 inhibitor compound or pharmaceutically acceptable salt or ester or solvate thereof and a preparation method and application of the piperidine USP7 inhibitor compound or pharmaceutically acceptable salt or ester or solvate thereof. The compound provided by the invention can inhibit the activity of USP7 enzyme, has very good selectivity and druggability, and can be used for preparing medicines for preventing or treating tumor diseases or virus infectious diseases.
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Paragraph 0598-0601
(2021/04/07)
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- Biphenyl compound as well as preparation method and medical application thereof
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The invention discloses a biphenyl compound as well as a preparation method and medical application thereof, the structure of the biphenyl compound is shown as a formula (I) or a formula (II), and thebiphenyl compound or pharmaceutically acceptable salt, tautomer, meso-isomer, raceme, stereoisomer, metabolite, metabolite precursor, prodrug or solvate thereof is a PD-L1 inhibitor. The compound hasa remarkable inhibiting effect on the interaction of PD-1 and PD-L1 protein, so that the compound can be applied to the preparation of PD-L1 inhibitors and immunomodulator drugs for preventing or treating tumors, autoimmune diseases, organ transplant rejection, infectious diseases and inflammatory diseases.
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Paragraph 0414-0420
(2020/11/22)
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- Adjusting the lipid-water distribution coefficient of iridium(iii) complexes to enhance the cellular penetration and treatment efficacy to antagonize cisplatin resistance in cervical cancer
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The effective design of metal complexes to manipulate their lipid-water distribution coefficient is an appealing strategy for improving their cellular penetration and treatment efficacy. Here, we conveniently synthesized three iridium (Ir) complexes with red fluorescence via the simple non-conjugate modification of the side arm of the ligand. Bio-evaluation revealed that upon adding non-conjugate selenium (Se) arene derivatives, the lipid-water distribution coefficient of Ir-Se was found to be suitable, not only decreasing the toxic side effects of complexes to normal cells, but also effectively improving their anticancer activity via enhancing their penetration into tumor cells. Moreover, mechanistic investigations demonstrated that Ir-Se entered R-HeLa cells through endocytosis, and triggered apoptosis via the down-regulation of the mitochondrial membrane potential and excessive production of singlet oxygen, thereby possessing a highly effective cytotoxicity to antagonize cisplatin resistance. Therefore, we developed a convenient strategy to derive functional metal complexes and revealed that the introduction of Se on the side arm of the ligand provided the complexes with the capacity to reverse multidrug resistance.
- Chen, Tianfeng,Chen, Zhen,Feng, Pengju,Hou, Liyuan,Huang, Wei,Li, Yiqun
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supporting information
p. 11556 - 11564
(2020/09/07)
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- Palladium-Catalyzed Methylation of Aryl, Heteroaryl, and Vinyl Boronate Esters
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A method for the direct methylation of aryl, heteroaryl, and vinyl boronate esters is reported, involving the reaction of iodomethane with aryl-, heteroaryl-, and vinylboronate esters catalyzed by palladium and PtBu2Me. This transformation occurs with a remarkably broad scope and is suitable for late-stage derivatization of biologically active compounds via the boronate esters. The unique capabilities of this method are demonstrated by combining carbon-boron bond-forming reactions with palladium-catalyzed methylation in a tandem transformation.
- Haydl, Alexander M.,Hartwig, John F.
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supporting information
p. 1337 - 1341
(2019/02/26)
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- Endothelin antagonists benzene oxygen benzene acetic acids and its preparation method and application
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The invention provides a phenoxy phenylacetic acid endothelin antagonist shown in a formula (I) or a pharmaceutically acceptable salt thereof, and also provides a preparation method of the benzene oxygen phenylacetic acid endothelin antagonist or the pharmaceutically acceptable salt thereof, and an application thereof in preparation of a medicament for treating cardiovascular and cerebrovascular diseases, tumors, diabetes mellitus, nephrosis, asthma or hyperthyroidism.
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Paragraph 0065-0067
(2016/11/02)
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- Synthesis and photovoltaic properties of two-dimensional copolymers based on novel benzothiadiazole and quinoxaline acceptors with conjugated dithienylbenzothiadiazole pendants
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Two novel acceptors of benzo[c][1,2,5]thiadiazole and quinoxaline with conjugated dithienylbenzothiadiazole pendants were first designed and synthesized for building efficient photovoltaic copolymers. Based on benzo[1,2-b;3,4-b′]dithiophene donors and the
- Huang, Yuanshuai,Ye, Linglong,Wu, Fen,Mei, Suli,Chen, Huajie,Tan, Songting
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p. 668 - 677
(2016/02/09)
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- Discovery of phenoxybutanoic acid derivatives as potent endothelin antagonists with antihypertensive activity
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A series of phenoxybutanoic acid derivatives were synthesized and tested for their antagonistic activity on the contraction of the rat thoracic aortic ring induced by endothelin-1. Preliminary screening results showed that 6e and 6g with benzoheterocycles demonstrated significant antagonistic activities when compared to the reference compound BQ123. The results from additional assays for the binding affinity and selectivity for endothelin receptors showed that 6e was a selective ETA antagonist with a nanomolar IC50. Moreover, 6e was effective in relieving hypoxia-induced pulmonary arterial hypertension and right ventricular weight ratio. Therefore, 6e may have potential for further development as a therapeutic agent for the treatment of cardiovascular diseases.
- Cai, Jin,Liu, Ligang,Hong, Kwon Ho,Wang, Peng,Li, Lushen,Cao, Meng,Sun, Chunlong,Wu, Xiaoqing,Zong, Xi,Chen, Junqing,Ji, Min
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p. 657 - 667
(2015/02/19)
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- Sulphur Nitrides in Organic Chemistry. Part 16. The Reaction of Tetrasulphur Tetranitride with Alkyl- and Alkylhalophenols. Preparation of 2,1,3-Benzothiadiazoles.
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The reaction of tetrasulphur tetranitride (N4S4) with alkylphenols 1a-o and alkylhalophenols 2a-i gave the corresponding 2,1,3-benzothiadiazoles 3a-n in 12-84percent yields.The reaction with 2,6-di-t-butylphenols 1p, q and 2j afforded N,N'-thiobis(1,4-ben
- Mataka, Shuntaro,Takahashi, Kazufumi,Shiwaku, Sohgo,Tashiro, Masashi
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p. 3649 - 3665
(2007/10/02)
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