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Benzenesulphonamide

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Chemical Structure| 98-10-2 同义名 : Phenyl sulfonamide;Benzenesulfonamide;Benzosulfonamide
CAS号 : 98-10-2
货号 : A119509
分子式 : C6H7NO2S
纯度 : 98%
分子量 : 157.19
MDL号 : MFCD00007930
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(667.98 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Carbonic Anhydrase
描述 Benzenesulfonamide is an inhibitor of human carbonic anhydrase B. Benzenesulfonamide derivatives are effective in the treatment of proliferative diseases such as cancer. Infection of HeLa cells was significantly inhibited by the oxazole-benzenesulfonamides, and the antiviral activity was most potent against replication stages before 8 h postinfection. Benzenesulfonamide inhibit intracellular HIV-1 reverse transcription and replication of WT HIV-1, as well as HIV-1 mutants that are resistant to current RT (reverse transcriptase) inhibitors[3]. In vivo anti-inflammatory evaluation revealed that benzenesulfonamides bearing pyrazole moiety 19, 20 and its cyclized form 23 exhibited the highest anti-inflammatory activity with comparable potency to celecoxib. Benzenesulfonamide derivatives 19 and 20 displayed higher predicted binding affinities inside the COX-2 active site[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01729923 Recurrent Colon Carcinoma ... 展开 >> Recurrent Rectal Carcinoma Stage IVA Colon Cancer Stage IVA Rectal Cancer Stage IVB Colon Cancer Stage IVB Rectal Cancer 收起 << Phase 2 Terminated(Funding ended) - United States, Washington ... 展开 >> Fred Hutch/University of Washington Cancer Consortium Seattle, Washington, United States, 98109 收起 <<
NCT03403634 Metastatic Carcinoma in the Li... 展开 >>ver Recurrent Colorectal Carcinoma Stage IV Colorectal Cancer AJCC v7 Stage IVA Colorectal Cancer AJCC v7 Stage IVB Colorectal Cancer AJCC v7 收起 << Early Phase 1 Recruiting December 1, 2019 United States, New York ... 展开 >> Roswell Park Cancer Institute Recruiting Buffalo, New York, United States, 14263 Contact: Patrick M. Boland    716-845-1912    Patrick.Boland@roswellpark.org    Principal Investigator: Patrick M. Boland 收起 <<
NCT03599453 Triple -Negative Breast Cancer... 展开 >> Estrogen Receptor Negative HER2/Neu Negative Anatomic Stage IV Breast Cancer AJCC Progesterone Receptor Negative 收起 << Phase 2 Not yet recruiting July 2022 -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

6.36mL

1.27mL

0.64mL

31.81mL

6.36mL

3.18mL

63.62mL

12.72mL

6.36mL
参考文献

[1]Kumar R, Bua S, et al. Benzenesulfonamide bearing imidazothiadiazole and thiazolotriazole scaffolds as potent tumor associated human carbonic anhydrase IX and XII inhibitors. Bioorg Med Chem. 2017 Feb 1;25(3):1286-1293.

[2]Rutkauskas K, Zubriene A, et al. 4-amino-substituted benzenesulfonamides as inhibitors of human carbonic anhydrases. Molecules. 2014 Oct 28;19(11):17356-80.

[3]Rawle DJ, Li D, Wu Z, et al. Oxazole-Benzenesulfonamide Derivatives Inhibit HIV-1 Reverse Transcriptase Interaction with Cellular eEF1A and Reduce Viral Replication. J Virol. 2019;93(12):e00239-19. Published 2019 May 29

[4]Taher ES, Ibrahim TS, Fares M, et al. Novel benzenesulfonamide and 1,2-benzisothiazol-3(2H)-one-1,1-dioxide derivatives as potential selective COX-2 inhibitors. Eur J Med Chem. 2019;171:372-382