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Wu, C., Decker, E.R., Blok, N., Bui, H., You, T.J., Wang, J., Bourgoyne, A.R., Knowles, V., Berens, K.L., Holland, G.W., Brock, T.A. and Dixon, R.A.F. (2004) Discovery, Modeling, and Human Pharmacokinetics of N-(2-Acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a Second Generation, ET A Selective, and Orally Bioavailable Endothelin Antagonist 1. Journal of Medicinal Chemistry, 47, 1969-1986.
http://dx.doi.org/10.1021/jm030528p
has been cited by the following article:
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TITLE:
New Approaches for the Use of Acetoacetanilide in the Synthesis of Thiophenes and Their Fused Derivatives with Anti-Tumor Activity
AUTHORS:
Rafat M. Mohareb, Sherif M. Sherif, Wagnat W. Wardakhan, Amr S. Abouzied
KEYWORDS:
Acetoaceanilide, Thiophene, Anti-Tumor, Docking
JOURNAL NAME:
Open Access Library Journal,
Vol.1 No.8,
November
26,
2014
ABSTRACT: Acetoacetanilide derivatives 1a-c reacted with either malnonitrile or ethyl cyanoacetate and elemental sulfur to give the thiophene derivatives 3a-f. The reactivity of 3a towards some chemical reagents to give thiophene, theino[2,3-b]pyridine, thieno[2,3-c]pyrimidine and coumarin derivatives was studied. The anti-tumor evaluation of the newly synthesized compounds against the three human tumor cells lines namely breast adenocarcinoma (MCF-7), non-small cell lung cancer (NCI-H460) and CNS cancer (SF-268) showed that compounds 8a, 8b and 14 exhibit higher inhibitory effects towards the three tumor cell lines than the positive control doxorubicin.
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