Synthesis, antitumor activity and molecular docking study of novel Sulfonamide-Schiff's bases, thiazolidinones, benzothiazinones and their C-nucleoside derivatives

被引：159

作者：

Kamel, Mohsen M. ^{[1
]}

Ali, Hamed I. ^{[2
]}

Anwar, Manal M. ^{[1
]}

Mohamed, Neama A. ^{[1
]}

Soliman, AbdelMohsen M. ^{[1
]}

机构：

[1] Natl Res Ctr, Dept Med Chem, Cairo, Egypt

[2] Helwan Univ, Fac Pharm, Dept Pharmaceut Chem, Helwan, Egypt

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 02期

关键词：

Sugar-Schiff's base; Thiazolidin-4-one; Benzothiazin-4-one; Antitumor activity; Autodock; Protein tyrosine kinase; POTENTIAL ANTICANCER AGENTS;

D O I：

10.1016/j.ejmech.2009.10.044

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of sulfapyridine-polyhydroxyalkylidene (or arylidene)-imino derivatives (Schiff's bases) 2a-c and 4a-e were prepared by condensation of 4-amino-N-pyridin-2-ylbenzenesulfonamide (1) with different monosaccharides or with aromatic aldehydes. Treatment of 2a-c with thioglycolic acid led to the formation of the C-nucleosides (3a-c), while treatment of 4a-e with thioglycolic and/or thiosalicylic acids afforded the corresponding 2-arylthiazolidin-4-one or 2-arylbenzothiazin-4-one derivatives 5a-e and/or 6a-e, respectively. Some representative examples of the newly prepared compounds showed considerable cytotoxic effect against breast carcinoma cell line MCF7 and cervix carcinoma cell line HEIA in comparison with 5-flurouracil and doxorubicin. AutoDock molecular docking into PTK has been done for lead optimization of the compounds in study as potential PTK inhibitors. (C) 2009 Elsevier Masson SAS. All rights reserved.

引用

页码：572 / 580

页数：9

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