Abstract

A set of substituted sulfadiazine compounds was prepared as cytotoxic and antitumor agents by using 4-amino-N-(pyrimidin-2-yl)benzenesulfonamide (1) as the starting material. Compound 1 was reacted with different reagents to give the corresponding sulfadiazines 2-18 and hydrozaones 19a-h which were evaluated for their in vitro cytotoxicity versus four cancer cell lines. Compounds 3, 5, 19d and 19h were active against the tested cancer cells.

Highlights

  • Sulfonamides have numerous biological actions, such as antibacterial,[1] hypoglycemia,[2] diuretic,[3] anti-carbonic anhydrase[3,4] and antithyroid.[5]

  • The first goal in this realization is to synthesis several novel structures having anticancer action and the second goal is to exam the effect of the substitution of pyridine, pyrimidine, oxadiazole, and azo derivatives on the anticancer action and to research their structure action relationships

  • The MS spectra of sulfonamides 2–4 offered the molecular weight at m/z 378 (M+–2) and at m/z 423

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Summary

Introduction

Sulfonamides have numerous biological actions, such as antibacterial,[1] hypoglycemia,[2] diuretic,[3] anti-carbonic anhydrase[3,4] and antithyroid.[5].

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