- Design and synthesis of chromone-nitrogen mustard derivatives and evaluation of anti-breast cancer activity
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Chromone has emerged as one of the most important synthetic scaffolds for antitumor activity, which promotes the development of candidate drugs with better activity. In this study, a series of nitrogen mustard derivatives of chromone were designed and syn
- Sun, Jianan,Mu, Jiahui,Wang, Shenglin,Jia, Cai,Li, Dahong,Hua, Huiming,Cao, Hao
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p. 431 - 444
(2022/01/04)
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- Design and synthesis of β-carboline derivatives with nitrogen mustard moieties against breast cancer
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To discover the promising antitumor agents, a series of β-carboline derivatives with nitrogen mustard moieties were designed and synthesized. Most target derivatives showed antiproliferative activity against MCF-7 and MDA-MB-231 cells. Among them, (1-meth
- Bai, Jiao,Cao, Hao,Hu, Xu,Hua, Huiming,Li, Dahong,Sun, Jianan,Wang, Jiesen,Wang, Xinyan
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- Novel hybrids of natural oridonin-bearing nitrogen mustards as potential anticancer drug candidates
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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.
- Xu, Shengtao,Pei, Lingling,Wang, Chengqian,Zhang, Yun-Kai,Li, Dahong,Yao, Hequan,Wu, Xiaoming,Chen, Zhe-Sheng,Sun, Yijun,Xu, Jinyi
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p. 797 - 802
(2014/08/05)
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- Gem-diphosphonic acids, and pharmaceutical compositions containing them
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Diphosphonic acids of formula (I), wherein R1 and R2 are hydrogen or C1 -C4 alkyl; (A) is hydrogen, halogen, hydroxy or C1 -C12 alkyl; (B) is a bond, a C1 -C8 alkylene chain, a cycloalkylalkylene chain, an alkylene chain substituted by cyclohexyl or cyclopentyl groups, or an aralkyl chain, an alkyl chain containing an heteroatom (O, S or N--CH3) or an ureido residue --(CH2)nl --NHCONH--(CH2)n --with n ranging from 1 to 5, R3 is hydrogen, C1 -C9 alkyl, C3 -C6 cycloalkyl, benzyl, phenyl or p-methoxybenzyl; (C) is C1 -C5 alkyl, phenyl or an aralkyl chain; R4 is hudrogen, C1 -C5 alkyl or an amino group optionally substituted by alkyl, phenyl, benzyl, p-methoxybenzyl, acyl, amminoacidic or peptide groups; R5 and R6 are 2-haloethyl or together form a 1-aziridinyl residue, are useful as antitumor agent.
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