Synthesis and antitumor activity of ATB-429 derivatives containing a nitric oxide-releasing moiety

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• 作者：Chunlan Wang^a ; ^&dagger ; ; Guimin Xia^a ; ^&dagger ; ; Xiujun Liu^a ; ^{liuxiujun2000@163.com" class="auth_mail" title="E-mail the corresponding author} ; Rui Zhang^a ; Yun Chai^a ; Jun Zhang^a ; ^b ; Xiaoning Li^a ; Yang Yang^a ; Juxian Wang^a ; Mingliang Liu^a ; ^{lmllyx@126.com" class="auth_mail" title="E-mail the corresponding author}
• 关键词：VJRZZAUSRQHVAB-UHFFFAOYSA-N ; FLTVEWINZQQISY-UHFFFAOYSA-N ; NKSSHCIJJUSHTI-UHFFFAOYSA-N ; FRXDVDHWFLUAMW-UHFFFAOYSA-N ; PLQJDZREQJCQAP-UHFFFAOYSA-N ; WAFAULTYESCLRC-UHFFFAOYSA-N ; JXFQAABXOJURSK-UHFFFAOYSA-N ; BTQLKFMADUDCQO-UHFFFAOYSA-N ; LNVYUTKBSPJEOM-UHFFFAOYSA-N ; UKGGQDHEDIPBLM-UHFFFAOYSA-N ; OILHLKALMUGQKS-UHFFFAOYSA-N ; SPVKGHROWFKJLZ-UHFFFAOYSA-N ; MABGNYLWOIBKOV-UHFFFAOYSA-N
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 May 2016
• 年：2016
• 卷：26
• 期：9
• 页码：2355-2359
• 全文大小：488 K

文摘

A series of novel ATB-429 (an anti-inflammatory candidate) derivatives containing a nitric oxide (NO)-releasing moiety were designed, synthesized and evaluated for their in vitro activity against six human cancer cell lines. Our results reveal that phenylsulfonylfuroxan-based derivatives have considerable antitumor activity, and compounds 7–9 (IC₅₀s: 0.256–3.024 μM) against HT-29 and PANC-1, 8a,b (IC₅₀s: 2.677–3.051 μM) against MCF-7 and 8a (IC₅₀: 1.270 μM) against DU145 are more active than Vandetanib (IC₅₀s: 1.925–4.107 μM).