Novel Sophoridine Derivatives Bearing Phosphoramide Mustard Moiety Exhibit Potent Antitumor Activities In Vitro and In Vivo

Novel mustard functionalized sophoridine derivatives were synthesized and evaluated for their cytotoxicity against of a panel of various cancer cell lines. They were shown to be more sensitive to S180 and H22 tumor cells with IC50 values ranging from 1.01–3.65 μM, and distinctly wer...

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Main Authors:	Dongdong Li, Linlin Dai, Xiumei Zhao, Shuang Zhi, Hongsheng Shen, Zibo Yang
Format:	Article
Language:	English
Published:	MDPI AG 2018-08-01
Series:	Molecules
Subjects:	mustard functionalized sophoridine derivatives antitumor activity apoptosis
Online Access:	http://www.mdpi.com/1420-3049/23/8/1960

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spelling	doaj-2e8539bebf3e429288b211ea538f61d12020-11-25T01:41:02ZengMDPI AGMolecules1420-30492018-08-01238196010.3390/molecules23081960molecules23081960Novel Sophoridine Derivatives Bearing Phosphoramide Mustard Moiety Exhibit Potent Antitumor Activities In Vitro and In VivoDongdong Li0Linlin Dai1Xiumei Zhao2Shuang Zhi3Hongsheng Shen4Zibo Yang5Tianjin Institute of Medical and Pharmaceutical Sciences, Tianjin 300020, ChinaTianjin Institute of Medical and Pharmaceutical Sciences, Tianjin 300020, ChinaTianjin Institute of Medical and Pharmaceutical Sciences, Tianjin 300020, ChinaTianjin Institute of Medical and Pharmaceutical Sciences, Tianjin 300020, ChinaTianjin Institute of Medical and Pharmaceutical Sciences, Tianjin 300020, ChinaTianjin Institute of Medical and Pharmaceutical Sciences, Tianjin 300020, ChinaNovel mustard functionalized sophoridine derivatives were synthesized and evaluated for their cytotoxicity against of a panel of various cancer cell lines. They were shown to be more sensitive to S180 and H22 tumor cells with IC50 values ranging from 1.01–3.65 μM, and distinctly were more cytotoxic to cancer cells than normal cell L929. In addition, compounds 7a, 7c, and 7e displayed moderate tumor suppression without apparent organ toxicity in vivo against mice bearing H22 liver tumors. Furthermore, they arrested tumor cells in the G1 phase and induced cellular apoptosis. Their potential binding modes with DNA-Top I complex have also been investigated.http://www.mdpi.com/1420-3049/23/8/1960mustard functionalized sophoridine derivativesantitumor activityapoptosis
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Dongdong Li Linlin Dai Xiumei Zhao Shuang Zhi Hongsheng Shen Zibo Yang
spellingShingle	Dongdong Li Linlin Dai Xiumei Zhao Shuang Zhi Hongsheng Shen Zibo Yang Novel Sophoridine Derivatives Bearing Phosphoramide Mustard Moiety Exhibit Potent Antitumor Activities In Vitro and In Vivo Molecules mustard functionalized sophoridine derivatives antitumor activity apoptosis
author_facet	Dongdong Li Linlin Dai Xiumei Zhao Shuang Zhi Hongsheng Shen Zibo Yang
author_sort	Dongdong Li
title	Novel Sophoridine Derivatives Bearing Phosphoramide Mustard Moiety Exhibit Potent Antitumor Activities In Vitro and In Vivo
title_short	Novel Sophoridine Derivatives Bearing Phosphoramide Mustard Moiety Exhibit Potent Antitumor Activities In Vitro and In Vivo
title_full	Novel Sophoridine Derivatives Bearing Phosphoramide Mustard Moiety Exhibit Potent Antitumor Activities In Vitro and In Vivo
title_fullStr	Novel Sophoridine Derivatives Bearing Phosphoramide Mustard Moiety Exhibit Potent Antitumor Activities In Vitro and In Vivo
title_full_unstemmed	Novel Sophoridine Derivatives Bearing Phosphoramide Mustard Moiety Exhibit Potent Antitumor Activities In Vitro and In Vivo
title_sort	novel sophoridine derivatives bearing phosphoramide mustard moiety exhibit potent antitumor activities in vitro and in vivo
publisher	MDPI AG
series	Molecules
issn	1420-3049
publishDate	2018-08-01
description	Novel mustard functionalized sophoridine derivatives were synthesized and evaluated for their cytotoxicity against of a panel of various cancer cell lines. They were shown to be more sensitive to S180 and H22 tumor cells with IC50 values ranging from 1.01–3.65 μM, and distinctly were more cytotoxic to cancer cells than normal cell L929. In addition, compounds 7a, 7c, and 7e displayed moderate tumor suppression without apparent organ toxicity in vivo against mice bearing H22 liver tumors. Furthermore, they arrested tumor cells in the G1 phase and induced cellular apoptosis. Their potential binding modes with DNA-Top I complex have also been investigated.
topic	mustard functionalized sophoridine derivatives antitumor activity apoptosis
url	http://www.mdpi.com/1420-3049/23/8/1960
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Novel Sophoridine Derivatives Bearing Phosphoramide Mustard Moiety Exhibit Potent Antitumor Activities In Vitro and In Vivo

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