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Synthesis and Cytotoxic Activity of Indolo[2,3-a]Pyrrolo[3,4-c]Carbazole-5,7-Dione N-Glycosides Substituted on the Maleimide Nitrogen Atom
Pharmaceutical Chemistry Journal ( IF 0.8 ) Pub Date : 2020-08-01 , DOI: 10.1007/s11094-020-02222-x
L. V. Ektova , V. A. Eremina , N. I. Tikhonova , I. L. Plikhtyak , L. A. Medvedeva , I. V. Yartseva , N. I. Moiseeva , I. S. Golubeva , I. P. Yavorskaya , A. P. Bud’ko , O. I. Tarasova , R. B. Pugacheva

Reactions of indolo[2,3-a]furano[3,4-c]carbazole-5,7-diones with hydrazine hydrate, hydroxylamine hydrochloride, and formyl hydrazine produced the corresponding N-6-substituted indolopyrrolocarbazole glycosides with the carbohydrate residues L-arabinose, D-galactose, D-xylose, and D-ribose. The obtained compounds were studied in vitro and in vivo and showed significant antiproliferative activity against HCT-116 cells (IC50 = 10–6 – 10–7 M) and high antitumor effects on Ehrlich ascites tumor and P-388 lymphocytic leukemia models. The lifespan increase of animals in the first model ranged from 540 – 495% to 172 – 132%; in the second model, from 80 – 83% to 120 – 93%.

中文翻译:

马来酰亚胺氮原子上取代的吲哚[2,3-a]吡咯并[3,4-c]咔唑-5,7-二酮N-糖苷的合成及细胞毒活性

吲哚[2,3-a]呋喃并[3,4-c]咔唑-5,7-二酮与水合肼、盐酸羟胺和甲酰肼的反应产生相应的N-6-取代吲哚并吡咯咔唑糖苷和碳水化合物残基L -阿拉伯糖、D-半乳糖、D-木糖和D-核糖。获得的化合物在体外和体内进行了研究,并显示出对 HCT-116 细胞的显着抗增殖活性(IC50 = 10–6 – 10–7 M)和对 Ehrlich 腹水肿瘤和 P-388 淋巴细胞白血病模型的高抗肿瘤作用。第一个模型中动物的寿命增加范围从 540 – 495% 到 172 – 132%;在第二个模型中,从 80 – 83% 到 120 – 93%。
更新日期:2020-08-01
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