Antitumor agents 259. Design, syntheses, and structure-activity relationship study of desmosdumotin C analogs.

Antitumor agents 259. Design, syntheses, and structure-activity relationship study of desmosdumotin C analogs. Research Abstract Details 

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Antitumor agents 259. Design, syntheses, and structure-activity relationship study of desmosdumotin C analogs. Abstract Text:

Kyoko Nakagawa-Goto,Tzu-Hsuan Chen,Chieh-Yu Peng,Kenneth F Bastow,Jiu-Hong Wu,Kuo-Hsiung Lee,

Desmosdumotin C (1) and its analogs previously showed potent, selective in vitro anticancer activity. To explore structure-activity relationships of 1 and further increase potency and selectivity, 15 novel analogs (7-15 and 21-26) were synthesized and evaluated for cytotoxity against several human tumor cell lines, as well as inhibition of human endothelial (HUVEC) replication. 4-Bromo-3',3',5'-tripropyl analog 26 showed significant cytotoxity against A549, A431, 1A9, and HCT-8 with ED50 values of 1.0, 1.2, 0.9, and 1.3 mug/mL, respectively. Compound 26 also strongly inhibited the growth of matched tumor cells, KB-VIN and its parent cell KB. Furthermore, analogs 13 and 21 were over 5-fold more potent against KB-VIN than KB. Bromination of ring-B and tripropyl functionalization of ring-A enhanced activity, while alkylation of ring-B promoted KB-VIN/KB selectivity. 2-Furyl analog 16 showed selective activity against HUVEC, suggesting that it may have potential as a new prototype for angiogenesis inhibition.

Antitumor agents 259. Design, syntheses, and structure-activity relationship study of desmosdumotin C analogs. Publishing Authors By Initials

K Nakagawa-Goto,TH Chen,CY Peng,KF Bastow,JH Wu,KH Lee,

For similar biochemical phenomena, metabolism, and nutrition: biochemical phenomena: structure-activity relationship research abstracts see: biochemical phenomena, metabolism, and nutrition: biochemical phenomena: structure-activity relationship research

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Antitumor agents 259. Design, syntheses, and structure-activity relationship study of desmosdumotin C analogs. Journal Published:

PUBLICATION TYPE: Research Support, Non-U.S. Gov

Journal: Journal of medicinal chemistry

VOLUME: 50

Page Numbers: 3354-8

Journal Abbreviation: J. Med. Chem.

ISSN: 0022-2623

DAY: 15

MONTH: 06

YEAR: 2007

Antitumor agents 259. Design, syntheses, and structure-activity relationship study of desmosdumotin C analogs. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 9716531

Antitumor agents 259. Design, syntheses, and structure-activity relationship study of desmosdumotin C analogs. Keywords Mesh Terms:

KEYWORDS: Structure-Activity Relationship

MESH TERMS: pharmacology

Chemical & Substance for Abstract: Antitumor agents 259. Design, syntheses, and structure-activity relationship study of desmosdumotin C analogs. Information

Substance Name: desmosdumotin C

Registry Number: 0

Grant and Affiliation Information for Antitumor agents 259. Design, syntheses, and structure-activity relationship study of desmosdumotin C analogs.

AFFILIATION: Natural Products Research Laboratories, School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, USA.

Country: United States

AGENCY: United States NCI

GRANT: CA17625

ACRONYM: CA

MEDLINETA: J Med Chem

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