Singer Mathilde, Lopez Marie, Bornaghi Laurent F, Innocenti Alessio, Vullo Daniela, Supuran Claudiu T, Poulsen Sally-Ann
Eskitis Institute, Griffith University, Nathan, Queensland, Australia.
Bioorg Med Chem Lett. 2009 Apr 15;19(8):2273-6. doi: 10.1016/j.bmcl.2009.02.086. Epub 2009 Feb 26.
A series of benzene sulfonamides incorporating thio, sulfinyl or sulfonyl glycoside moieties were synthesized. These glycoconjugates were investigated for their ability to inhibit the enzymatic activity of four human carbonic anhydrases (hCA): isozymes I, II and tumour-associated isozymes IX and XII. The oxidation state of the sulfur in the carbohydrate tail moiety did not influence either enzyme inhibition potency or isozyme selectivity even though presenting opportunities for differing interactions with the target isozymes.
合成了一系列含有硫代、亚磺酰基或磺酰基糖苷部分的苯磺酰胺。研究了这些糖缀合物抑制四种人碳酸酐酶(hCA):同工酶I、II以及肿瘤相关同工酶IX和XII的酶活性的能力。碳水化合物尾部分中硫的氧化态即使为与靶同工酶进行不同相互作用提供了机会,也不会影响酶抑制效力或同工酶选择性。