68723-78-4Relevant articles and documents
Chromone 3-position nitric oxide donor derivative as well as preparation method and application thereof
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, (2021/05/05)
The invention relates to the fields of natural medicines and medicinal chemistry, and relates to a preparation method of a series of chromone 3-position nitric oxide donor derivatives with antitumor activity and a new application of the chromone 3-position nitric oxide donor derivatives in preparation of antitumor medicines. The chromone 3-position nitric oxide donor derivative and the pharmaceutically acceptable salt thereof are shown as a general formula I in the specification. Wherein R and R1 are described in the claims and the specification.
Chromone 2-position nitric oxide donor derivative as well as preparation method and application thereof
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, (2021/05/05)
The invention relates to the fields of natural medicines and medicinal chemistry, and relates to a preparation method of a series of chromone 2-position nitric oxide donor derivatives with antitumor activity and a new application of the chromone 2-position nitric oxide donor derivatives in preparation of antitumor medicines. The chromone 2-position nitric oxide donor derivative and the pharmaceutically acceptable salt thereof are shown as a general formula I in the specification. Wherein R and R1 are described in the claims and the specification.
Antiproliferative chromone derivatives induce K562 cell death through endogenous and exogenous pathways
Cao, Hao,Hua, Huiming,Huang, Xiaofang,Jiao, Runwei,Li, Dahong,Li, Haonan,Li, Zhanlin,Liu, Weiwei,Xu, Fanxing,Zang, Linghe
, p. 759 - 772 (2020/04/01)
A series of furoxan derivatives of chromone were prepared. The antiproliferative activities were tested against five cancer cell lines HepG2, MCF-7, HCT-116, B16, and K562, and two normal human cell lines L-02 and PBMCs. Among them, compound 15a exhibited the most potent antiproliferative activity. It was also found 15a produced more than 8 μM of NO at the peak time of 45 min by Griess assay. Generally, antiproliferative activity is positively related to NO release to some extent. Further in-depth studies on apoptosis-related mechanisms showed that 15a caused S-phase cell cycle arrest in a concentration-dependent manner and induced apoptosis significantly through mitochondria-related pathways. Human apoptosis protein array assay also demonstrated 15a increased the expression levels of pro-apoptotic Bax, Bad, HtrA2 and Trail R2/DR5. The expression of catalase and cell cycle blocker claspin were similarly up-regulated. In balance, 15a induced K562 cells death through both endogenous and exogenous pathways.