43088-00-2Relevant academic research and scientific papers
Design, synthesis, biological evaluation and in silico studies of few novel 2-substituted benzothiazole derivatives as potential EGFR inhibitors
Mubeen, Muhammad,Kini, Suvarna Ganesh,Kumar, Avinash,Pai, Karkala Sreedhara Ranganath
, p. 961 - 971 (2019/10/28)
Background: There is a great unmet medical need for new anticancer small molecule therapeutics. Exhaustive literature review suggests that benzothiazole derivatives have good potential to exhibit anticancer activity. Compounds that inhibit the kinase acti
Synthesis and antitumor activity evaluation of new 2-(4-aminophenyl)benzothiazole derivatives bearing different heterocyclic rings
Yurtta?, Leyla,Tay, Funda,Demirayak, ?eref
, p. 458 - 465 (2015/07/23)
Twenty-five new N-[4-(benzothiazole-2-yl)phenyl]acetamide derivatives bearing different heterocyclic ring systems were synthesized using 2-(4-aminophenyl)benzothiazole structure as a pharmacophoric group. Final compounds were screened for their potential
An efficient one-pot synthesis of benzothiazolo-4β-anilino- podophyllotoxin congeners: DNA topoisomerase-II inhibition and anticancer activity
Kamal, Ahmed,Kumar, B. Ashwini,Suresh, Paidakula,Shankaraiah, Nagula,Kumar, M. Shiva
scheme or table, p. 350 - 353 (2011/02/27)
An efficient one-pot iodination methodology for the synthesis of benzothiazolo-4β-anilino-podophyllotoxin (5a-h) and benzothiazolo-4β- anilino-4-O-demethylepipodophyllotoxin (6a-h) congeners has been successfully developed by using zirconium tetrachloride
N-substituted 2′-(aminoaryl)benzothiazoles as kinase inhibitors: Hit identification and scaffold hopping
Tasler, Stefan,Mueller, Oliver,Wieber, Tanja,Herz, Thomas,Krauss, Rolf,Totzke, Frank,Kubbutat, Michael H.G.,Schaechtele, Christoph
body text, p. 1349 - 1356 (2009/11/30)
Starting with a hit from vHTS attained by a docking procedure of virtual compounds into ATP pockets of different kinases applying the 4SCan technology, variations of the adenine mimic resulted in the identification of promising scaffolds, giving rise to in vitro IC50 values in the nanomolar range on different kinases down to 63 nM.
Substituted 2-arylbenzothiazoles as kinase inhibitors: Hit-to-lead optimization
Tasler, Stefan,Mueller, Oliver,Wieber, Tanja,Herz, Thomas,Pegoraro, Stefano,Saeb, Wael,Lang, Martin,Krauss, Rolf,Totzke, Frank,Zirrgiebel, Ute,Ehlert, Jan E.,Kubbutat, Michael H.G.,Schaechtele, Christoph
supporting information; experimental part, p. 6728 - 6737 (2009/12/09)
Based on an (aminoaryl)benzothiazole quinazoline hit structure for kinase inhibition, a systematic optimization program resulted in a lead structure allowing for inhibitory activities in cellular phosphorylation assays in the low nanomolar range.
2-arylbenzothiazole analogues and uses thereof
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Page/Page column 16, (2008/06/13)
The present invention relates to compounds of the general formula (I) and salts, prodrugs, and stereoisomers thereof, wherein Y independently represents S, O, NR2, SO, SO2; A independently represents a fife- or six-membered aromatic carbocycle or heterocycle and wherein R1 to R20 in formula (I) represent independently of each other a variety of different substituents comprising alkyl, aryl, aralkyl, alkylaryl, heteroaryl groups and monofunctional moieties.
2-Arylbenzothiazole analogues and uses thereof in the treatment of cancer
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Page/Page column 30-31, (2010/11/25)
The present invention relates to anticancer compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein Y independently represents S, O, NR 2 , SO, SO 2 ; A independently represents a five- or six-membered aromatic carbocycle or heterocycle and wherein R 1 in formula (I) represents one of the heteroaryl groups defined in the claims.
1H and 13C chemical shifts for 2-aryl and 2-N-arylamino benzothiazole derivatives
Billeau,Chatel,Robin,Faure,Galy
, p. 102 - 105 (2008/02/01)
The 1H and 13C NMR resonances for forty-three 2-aryl and 2-N-arylamino benzothiazole derivatives were completely assigned using a concerted application of one-and two-dimensional experiments (DEPT, gs-COSY, gs-HMQC and gs-HMBC). Copyright
Solid phase combinatorial synthesis of benzothiazoles and evaluation of topoisomerase II inhibitory activity
Choi, Suk-June,Park, Hyen Joo,Lee, Sang Kook,Kim, Sang Woong,Han, Gyoonhee,Choo, Hea-Young Park
, p. 1229 - 1235 (2007/10/03)
To investigate one possible mechanism of action of the cytotoxic activity of benzothiazoles, we synthesized 2-(substituted-phenyl)benzothiazoles and evaluated their ability to inhibit topoisomerase II activities. Solid phase combinatorial method using tri
Benzazole compounds
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, (2008/06/13)
There are disclosed herein benzazole compounds, exemplified by 2-(4-aminophenyl)benzothiazole and analogues or salts thereof, which exhibit very significant selective cytotoxic activity in respect of tumor cells, especially breast cancer cells, and which provide potentially useful chemotherapeutic agents for treatment of breast cancer.
