87936-09-2Relevant articles and documents
Novel hybrids of natural oridonin-bearing nitrogen mustards as potential anticancer drug candidates
Xu, Shengtao,Pei, Lingling,Wang, Chengqian,Zhang, Yun-Kai,Li, Dahong,Yao, Hequan,Wu, Xiaoming,Chen, Zhe-Sheng,Sun, Yijun,Xu, Jinyi
, p. 797 - 802 (2014)
A series of novel hybrids from natural product oridonin and nitrogen mustards were designed and synthesized to obtain more efficacious and less toxic antitumor agents. The antiproliferative evaluation showed that most conjugates were more potent than their parent compounds oridonin and clinically used nitrogen mustards against four human cancer cell lines (K562, MCF-7, Bel-7402, and MGC-803). Furthermore, the representative compounds 16a-c exhibited antiproliferative activities against the multidrug resistant cell lines (SW620/AD300 and NCI-H460/MX20). It was shown that the most effective compound 16b possesses a strong inhibitory activity with an IC50 value 21-fold lower than that of oridonin in MCF-7 cells and also exhibits selective cytotoxicity toward the cancer cells. Intriguingly, compound 16b has been demonstrated to significantly induce apoptosis and affect cell cycle progression in human hepatoma Bel-7402 cells.
Spirolactone type diterpene spliced hydrogen sulfide donor derivatives as well as preparation method and application thereof
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, (2020/09/16)
The invention relates to the field of natural medicines and medicinal chemistry, and relates to spirolactone diterpene spliced hydrogen sulfide donor derivatives as well as a preparation method and application thereof. The invention particularly relates to the preparation method of a series of spirolactone type kaurane diterpene hydrogen sulfide donor derivatives with anti-tumor activity and the application of the derivatives in preparation of anti-tumor drugs. The spirolactone type diterpene hydrogen sulfide donor derivatives and the pharmaceutically acceptable salts thereof are represented by a general formula I or II, wherein R is as described in the claims and the specification.
Hydrogen sulfide donating ent-kaurane and spirolactone-type 6,7-seco-ent-kaurane derivatives: Design, synthesis and antiproliferative properties
Li, Haonan,Gao, Xiang,Huang, Xiaofang,Wang, Xianhua,Xu, Shengtao,Uchita, Takahiro,Gao, Ming,Xu, Jinyi,Hua, Huiming,Li, Dahong
, p. 446 - 457 (2019/06/18)
Motivated by our interest in hydrogen sulfide bio-chemistry and ent-kaurane diterpenoid chemistry, 14 hydrogen sulfide donating derivatives (9, 11a-c, 12a-c, 13, 14, 16a-c and 17a-b) of ent-kaurane and spirolactone-type 6,7-seco-ent-kaurane were designed and synthesized. Four human cancer cell lines (K562, Bel-7402, SGC-7901 and A549) and two normal cell lines (L-02 and PBMC) were selected for antiproliferative assay. Most derivatives showed more potent activities than the lead ent-kaurane oridonin. Among them, compound 12b exhibited the most potent antiproliferative activities, with IC50 values of 1.01, 0.88, 4.36 and 5.21 μM against above human cancer cell lines, respectively. Further apoptosis-related mechanism study indicated that 12b could arrest Bel-7402 cell cycle at G1 phase and induce apoptosis through mitochondria related pathway. Through Western blot assay, 12b was shown to influence the intrinsic pathway by increasing the expression of Bax, cleaved caspase-3, cytochrome c and cleaved PARP, meanwhile suppressing procaspase-3, Bcl-2, Bcl-xL and PARP.
