Synthesis and Biological Evaluation N-(6,7-dimethoxynaphthalen-yl) sulfamide Derivatives as Novel Inhibitors of Angiogenesis and Tumor Growth

Abstract

Target compounds were synthesized by the experiment process in Scheme 1. Firstly, mesyl groups were introduced into naphthalene-2,3-diol in presence of triethylamine and dichloromethane (DCM). Secondly, the nitro group was introduced in the circumstances with nitric acid and acetic anhydride. Thirdly, the two sulfonyl groups on compound 3 were eliminated by dimethyl sulfate and sodium hydroxide solution [32]. Then the nitro-group on compound 4 was deoxidized to the amino group by Pd-C/H 2 in methanol solution to give compound 5 [33], which was treated with various substituted sulfonyl chlorides to generate compounds XGS-1 to XGS-15 [34]. Analytic and spectral of the whole series compounds are in total accordance to the proposed structures.

Role of heterocycles in inhibition of VEGFR-2 – a recent update (2019–2022)

“…Evidence-based establishment of the pyridine nucleus as an antitumor agent 40,41 and increasing employment of naphthalene scaffolds in anticancer drug design 42,43 inspired Abdelhaleem et al to design and synthesize a series of naphthalene-containing pyridine derivatives. 44 In initial anticancer activity, almost all the evaluated molecules demonstrated excellent activity.…”