69812-30-2Relevant articles and documents
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Faith
, p. 2063 (1947)
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cGAS ANTAGONIST COMPOUNDS
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Paragraph 0429, (2017/11/06)
Disclosed are novel compounds of Formula (I) that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.
Synthesis of sulofenur analoges as antitumour agents: Part II
Youssef, Khairia M.,Al-Abdullah, Ebtihal,El-Khamees, Hamad
, p. 481 - 503 (2007/10/03)
A series of N-aryl-N′-heteroaryl or N,N′-diheteroaryl sulfonylurea has been prepared using two different methods. All the intermediates were prepared including heteroarylsulfonyl chlorides and aryl- or hetero-arylurea derivatives. Structural elucidation of the newly synthesized compounds were based on elementary analysis, IR, 1H & 1C NMR and mass spectra. The antitumor screening of the prepared compounds were performed at the National Cancer Institute (NCI) Bethesda, Maryland, USA. Compound N-(3-methylbenzothiazol-2-yl)-N′ -(1-benzodiazolyl-sulfonyl)urea (13) with GI50, TGI, LC50 (MG-MID) values of 25.1, 77.5, 93.3 μM, respectively is the most active compound in this study. It showed a broad spectrum antitumor activity as well as selective activity toward individual cell lines. It showed distinctive activities compared to that of sulofenur against RPMI-8226 leukemia, EKVX Non-small lung cancer, PC-3 prostate cancer, OVCAR-4 Ovarian cancer, CAKI-1Renal cancer, MDA-MB-435 and T-47D Breast cancer with GI50 values of 21.5, 1.7, 28.7, 25.9, 15.9, 27.9, 15.1 μM, respectively.