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Synthesis and structure-activity relationship study of water-soluble carbazole sulfonamide derivatives as new anticancer agents.
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2020-02-22 , DOI: 10.1016/j.ejmech.2020.112181 Yonghua Liu 1 , Yanbin Wu 1 , Lianqi Sun 1 , Yuxi Gu 1 , Laixing Hu 1
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2020-02-22 , DOI: 10.1016/j.ejmech.2020.112181 Yonghua Liu 1 , Yanbin Wu 1 , Lianqi Sun 1 , Yuxi Gu 1 , Laixing Hu 1
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Here, we formulated and investigated the structure-activity relationships of novel N-substituted carbazole sulfonamide derivatives with improved physicochemical properties. Most of these new compounds displayed good aqueous solubility. Certain molecules presented strong in vitro antiproliferative and in vivo antitumor activity. Relative to the control, 50 mg/kg compound 3v substantially reduced human HepG2 xenograft mouse tumor growth by 54.5% and its efficacy was comparable to that of CA-4P. Compound 3h demonstrated anticancer efficacy in both subcutaneous and orthotopic HepG2 xenograft mouse models. We also developed a novel synthetic method for 7-hydroxy-substituted carbazole sulfonamides. Compared with the control, 25 mg/kg compound 4c inhibited human HepG2 xenograft mouse tumor growth by 71.7% and was more potent than 50 mg/kg CA-4P with only 50% tumor shrinkage efficacy. Among the three water-soluble carbazole sulfonamide derivatives formulated in the present study, compound 4c displayed the most effective tumor growth inhibition in vivo and merit further investigation as potential antitumor agents for cancer therapy.
中文翻译：
新型水溶性咔唑磺酰胺衍生物的合成及构效关系研究。
在这里，我们制定并研究了具有改善的理化性质的新型N-取代咔唑磺酰胺衍生物的结构活性关系。这些新化合物大多数显示出良好的水溶性。某些分子具有很强的体外抗增殖和体内抗肿瘤活性。相对于对照，50 mg / kg化合物3v大大降低了人类HepG2异种移植小鼠肿瘤的生长54.5％，其功效与CA-4P相当。化合物3h在皮下和原位HepG2异种移植小鼠模型中均显示出抗癌功效。我们还开发了一种新型的7-羟基取代咔唑磺酰胺合成方法。与对照组相比，25 mg / kg化合物4c抑制人HepG2异种移植小鼠肿瘤的生长达71。浓度为7％，比50 mg / kg CA-4P更有效，肿瘤收缩率仅为50％。在本研究中配制的三种水溶性咔唑磺酰胺衍生物中，化合物4c在体内显示出最有效的肿瘤生长抑制作用，值得进一步研究作为潜在的抗癌药物进行癌症治疗。
更新日期：2020-02-23
中文翻译：
新型水溶性咔唑磺酰胺衍生物的合成及构效关系研究。
在这里，我们制定并研究了具有改善的理化性质的新型N-取代咔唑磺酰胺衍生物的结构活性关系。这些新化合物大多数显示出良好的水溶性。某些分子具有很强的体外抗增殖和体内抗肿瘤活性。相对于对照，50 mg / kg化合物3v大大降低了人类HepG2异种移植小鼠肿瘤的生长54.5％，其功效与CA-4P相当。化合物3h在皮下和原位HepG2异种移植小鼠模型中均显示出抗癌功效。我们还开发了一种新型的7-羟基取代咔唑磺酰胺合成方法。与对照组相比，25 mg / kg化合物4c抑制人HepG2异种移植小鼠肿瘤的生长达71。浓度为7％，比50 mg / kg CA-4P更有效，肿瘤收缩率仅为50％。在本研究中配制的三种水溶性咔唑磺酰胺衍生物中，化合物4c在体内显示出最有效的肿瘤生长抑制作用，值得进一步研究作为潜在的抗癌药物进行癌症治疗。
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