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Organoruthenium and Organoosmium Complexes of 2-Pyridinecarbothioamides Functionalized with a Sulfonamide Motif: Synthesis, Cytotoxicity and Biomolecule Interactions.
ChemPlusChem ( IF 3.0 ) Pub Date : 2018-06-19 , DOI: 10.1002/cplu.201800194
Jahanzaib Arshad 1, 2 , Muhammad Hanif 1 , Ayesha Zafar 1 , Sanam Movassaghi 1 , Kelvin K H Tong 1 , Jóhannes Reynisson 1 , Mario Kubanik 1 , Amir Waseem 2 , Tilo Söhnel 1 , Stephen M F Jamieson 3 , Christian G Hartinger 1
Affiliation  

Anticancer-active RuII -η6 -p-cymene complexes of bioactive 2-pyridinecarbothioamide ligands have been shown to have high selectivity for plectin and can be administered orally. Reported herein is the functionalization of a 2-pyridinecarbothioamide with a sulfonamide group and its conversion into M-η6 -p-cymene complexes (M = Ru, Os). The presence of a sulfonamide moiety in many organic drugs and metal complexes endows these agents with interesting biological properties and can transform the latter into multi-targeted agents. The compounds were characterized with standard methods and the in vitro anticancer activity data was compared with studies on the hydrolytic stability of the complexes and their reactivity to small biomolecules. A molecular modeling study revealed plausible modes of binding of the complexes in the catalytic pocket of carbonic anhydrase II.

中文翻译:

用磺酰胺基团官能化的2-吡啶碳硫代酰胺的有机钌和有机oo配合物:合成,细胞毒性和生物分子相互作用。

具有生物活性的2-吡啶基碳硫代酰胺酰胺配体的抗癌活性RuII-η6-β-cymene配合物已显示出对血凝素具有高选择性,可以口服给药。本文报道的是具有磺酰胺基团的2-吡啶基碳硫磺酰胺的官能化及其转化成M-η6-对-胞嘧啶配合物(M = Ru,Os)。许多有机药物和金属络合物中磺酰胺部分的存在使这些药物具有有趣的生物学特性,并且可以将后者转变为多目标药物。用标准方法对化合物进行了表征,并将体外抗癌活性数据与复合物的水解稳定性及其对小生物分子的反应性进行了研究。
更新日期:2018-06-19
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