79145-92-9Relevant academic research and scientific papers
Derivatives of nitrogen mustard anticancer agents with improved cytotoxicity
Antoni, Frauke,Bernhardt, Günther
, (2021)
In previous studies, we demonstrated that esters of bendamustine containing a basic moiety are far more cytotoxic anticancer agents than their parent compound and that the substitution of the labile ester moiety by a branched ester or an amide markedly in
Bivalent bendamustine and melphalan derivatives as anticancer agents
Scutaru, Ana Maria,Wenzel, Maxi,Gust, Ronald
, p. 1604 - 1615 (2011)
The alkylating agents bendamustine and melphalan are currently used in the treatment of various tumoral diseases. In order to increase their antitumor potency and tumor selectivity both compounds were integrated in structure-activity relationship studies
Design and synthesis of chromone-nitrogen mustard derivatives and evaluation of anti-breast cancer activity
Sun, Jianan,Mu, Jiahui,Wang, Shenglin,Jia, Cai,Li, Dahong,Hua, Huiming,Cao, Hao
, p. 431 - 444 (2022/01/04)
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
Design and synthesis of β-carboline derivatives with nitrogen mustard moieties against breast cancer
Bai, Jiao,Cao, Hao,Hu, Xu,Hua, Huiming,Li, Dahong,Sun, Jianan,Wang, Jiesen,Wang, Xinyan
, (2021/08/09)
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
Bifunctional cytotoxin and application thereof
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Paragraph 0040-0041, (2020/03/11)
The invention provides a bifunctional cytotoxin containing a duocarmycin analogue and a nitrogen mustard compound, and further provides an antibody drug conjugate coupled with the bifunctional cytotoxin and pharmaceutical application of the antibody drug
COMPOUNDS CONTAINING DEUTERIUM
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Page/Page column 26-28, (2020/05/21)
The invention provides a compound of formula (I), or a pharmaceutically acceptable salt thereof (Formula I), wherein, each R1-R30 is independently selected from the group consisting of H and deuterium, and at least one of R1/su
NOVEL FORMULATIONS COMPRISING MELFLUFEN
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Page/Page column 33-34, (2020/10/28)
The invention provides a pharmaceutical formulation comprising (or consisting essentially of) the following components: i) melflufen, or a salt thereof; ii) propylene glycol; iii) optionally one or more physiologically acceptable aqueous solvent(s); and i
Mechlorethamine quinolone derivative and preparing method and application thereof
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Paragraph 0026, (2019/06/07)
The invention relates to a mechlorethamine quinolone derivative (I). A preparing method of the derivative comprises the steps of firstly, conducting reduction and formylation on a quinolone compound to prepare 3-formyl quinolone (IV), and then carrying ou
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 (2014/08/05)
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.
Structure-based design, synthesis and biological testing of etoposide analog epipodophyllotoxin-N-mustard hybrid compounds designed to covalently bind to topoisomerase II and DNA
Yadav, Arun A.,Wu, Xing,Patel, Daywin,Yalowich, Jack C.,Hasinoff, Brian B.
, p. 5935 - 5949 (2015/02/02)
Drugs that target DNA topoisomerase II isoforms and alkylate DNA represent two mechanistically distinct and clinically important classes of anticancer drugs. Guided by molecular modeling and docking a series of etoposide analog epipodophyllotoxin-N-mustar
