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PDBsum entry 6ugr
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Lyase/lyase inhibitor
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PDB id
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6ugr
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References listed in PDB file
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Key reference
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Title
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&Quot;a sweet combination": developing saccharin and acesulfame k structures for selectively targeting the tumor-Associated carbonic anhydrases IX and XII.
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Authors
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S.Bua,
C.Lomelino,
A.B.Murray,
S.M.Osman,
Z.A.Alothman,
M.Bozdag,
H.A.Abdel-Aziz,
W.M.Eldehna,
R.Mckenna,
A.Nocentini,
C.T.Supuran.
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Ref.
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J Med Chem, 2020,
63,
321-333.
[DOI no: ]
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PubMed id
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Abstract
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The sweeteners saccharin (SAC) and acesulfame K (ACE) recently
entered the topic of anticancer human carbonic anhydrase (CA, EC 4.2.1.1)
inhibitors, as they showed to selectively inhibit the tumor-associated CAs
IX/XII over ubiquitous CAs. A drug design strategy is here reported, which took
SAC and ACE as leads and produced a series of
2H-benzo[e][1,2,4]thiadiazin-3(4H)-one-1,1-dioxides
(BTD). Many derivatives showed greater potency (
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