Antimalarial, antiproliferative, and antitumor activities of artemisinin-derived, chemically robust, trioxane dimers

Gary H. Posner; Poonsakdi Ploypradith; Michael H. Parker; Hardwin O'Dowd; Soon Hyung Woo; John Northrop; Mikhail Krasavin; Patrick Dolan; Thomas W. Kensler; Suji Xie; Theresa A. Shapiro

doi:10.1021/jm990363d

Antimalarial, antiproliferative, and antitumor activities of artemisinin-derived, chemically robust, trioxane dimers

Gary H. Posner, Poonsakdi Ploypradith, Michael H. Parker, Hardwin O'Dowd, Soon Hyung Woo, John Northrop, Mikhail Krasavin, Patrick Dolan, Thomas W. Kensler, Suji Xie, Theresa A. Shapiro

Research output: Contribution to journal › Article › peer-review

144 Scopus citations

Abstract

Nine C-10 non-acetal derivatives of the natural trioxane artemisinin (1) were prepared as dimers using some novel chemistry. As designed, each dimer was stable chemically. C-10 Olefinic dimers 7 and C-10 saturated dimers 8-13 all showed good to excellent antimalarial and antiproliferative activities in vitro. Dimers 8, 10, and 12 were especially potent and selective at inhibiting growth of some human cancer cell lines in the NCI in vitro 60-cell line assay.

Original language	English (US)
Pages (from-to)	4275-4280
Number of pages	6
Journal	Journal of medicinal chemistry
Volume	42
Issue number	21
DOIs	https://doi.org/10.1021/jm990363d
State	Published - 1999

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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title = "Antimalarial, antiproliferative, and antitumor activities of artemisinin-derived, chemically robust, trioxane dimers",

abstract = "Nine C-10 non-acetal derivatives of the natural trioxane artemisinin (1) were prepared as dimers using some novel chemistry. As designed, each dimer was stable chemically. C-10 Olefinic dimers 7 and C-10 saturated dimers 8-13 all showed good to excellent antimalarial and antiproliferative activities in vitro. Dimers 8, 10, and 12 were especially potent and selective at inhibiting growth of some human cancer cell lines in the NCI in vitro 60-cell line assay.",

author = "Posner, {Gary H.} and Poonsakdi Ploypradith and Parker, {Michael H.} and Hardwin O'Dowd and Woo, {Soon Hyung} and John Northrop and Mikhail Krasavin and Patrick Dolan and Kensler, {Thomas W.} and Suji Xie and Shapiro, {Theresa A.}",

year = "1999",

doi = "10.1021/jm990363d",

language = "English (US)",

volume = "42",

pages = "4275--4280",

journal = "Journal of medicinal chemistry",

issn = "0022-2623",

publisher = "American Chemical Society",

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TY - JOUR

T1 - Antimalarial, antiproliferative, and antitumor activities of artemisinin-derived, chemically robust, trioxane dimers

AU - Posner, Gary H.

AU - Ploypradith, Poonsakdi

AU - Parker, Michael H.

AU - O'Dowd, Hardwin

AU - Woo, Soon Hyung

AU - Northrop, John

AU - Krasavin, Mikhail

AU - Dolan, Patrick

AU - Kensler, Thomas W.

AU - Xie, Suji

AU - Shapiro, Theresa A.

PY - 1999

Y1 - 1999

N2 - Nine C-10 non-acetal derivatives of the natural trioxane artemisinin (1) were prepared as dimers using some novel chemistry. As designed, each dimer was stable chemically. C-10 Olefinic dimers 7 and C-10 saturated dimers 8-13 all showed good to excellent antimalarial and antiproliferative activities in vitro. Dimers 8, 10, and 12 were especially potent and selective at inhibiting growth of some human cancer cell lines in the NCI in vitro 60-cell line assay.

AB - Nine C-10 non-acetal derivatives of the natural trioxane artemisinin (1) were prepared as dimers using some novel chemistry. As designed, each dimer was stable chemically. C-10 Olefinic dimers 7 and C-10 saturated dimers 8-13 all showed good to excellent antimalarial and antiproliferative activities in vitro. Dimers 8, 10, and 12 were especially potent and selective at inhibiting growth of some human cancer cell lines in the NCI in vitro 60-cell line assay.

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DO - 10.1021/jm990363d

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SN - 0022-2623

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SP - 4275

EP - 4280

JO - Journal of medicinal chemistry

JF - Journal of medicinal chemistry

IS - 21

ER -

Antimalarial, antiproliferative, and antitumor activities of artemisinin-derived, chemically robust, trioxane dimers

Abstract

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