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

Abstract：

: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 HELA 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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Kamel MM,Ali HI,Anwar MM,Mohamed NA,Soliman AM

doi

10.1016/j.ejmech.2009.10.044

subject

Has Abstract

pub_date

2010-02-01 00:00:00

pages

572-80

issue

2

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(09)00546-7

journal_volume

45

pub_type

杂志文章

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