924708-48-5Relevant articles and documents
Aryl derivatives of 3H-1,2-benzoxathiepine 2,2-dioxide as carbonic anhydrase inhibitors
Pustenko, Aleksandrs,Nocentini, Alessio,Bala?ova, Anastasija,Alafeefy, Ahmed,Krasavin, Mikhail,?alubovskis, Raivis,Supuran, Claudiu T.
, p. 245 - 254 (2020)
A new series of homosulfocoumarins (3H-1,2-benzoxathiepine 2,2-dioxides) possessing various substitution patterns and moieties in the 7, 8 or 9 position of the heterocylic ring were prepared by original procedures and investigated for the inhibition of four physiologically relevant carbonic anhydrase (CA, EC 4.2.1.1) isoforms, the human (h) hCA I, II, IX and XII. The 8-substituted homosulfocoumarins were the most effective hCA IX/XII inhibitors followed by the 7-substituted derivatives, whereas the substitution pattern in position 9 led to less effective binders for the transmembrane, tumour-associated isoforms IX/XII. The cytosolic isoforms hCA I and II were not inhibited by these compounds, similar to the sulfocoumarins/coumarins investigated earlier. As hCA IX and XII are validated anti-tumour targets, with one sulphonamide (SLC-0111) in Phase Ib/II clinical trials, finding derivatives with better selectivity for inhibiting the tumour-associated isoforms over the cytosolic ones, as the homosulfocoumarins reported here, is of crucial importance.
Concise synthesis of rodgersinol and determination of the C-10 absolute configuration
Seo, Seung-Yong,Jung, Jong-Wha,Jung, Jae-Kyung,Kim, Nam-Jung,Chin, Young-Won,Kim, Jinwoong,Suh, Young-Ger
, p. 666 - 668 (2007/10/03)
Rodgersinol was synthesized via seven linear steps in 31% overall yield, and the absolute configuration of the C-10 stereogenic center was elucidated. The key feature of the synthesis involves the efficient Cu(II)-mediated coupling of two aromatic moietie