Antitumor agents. 256. Conjugation of paclitaxel with other antitumor agents: evaluation of novel conjugates as cytotoxic agents.

Antitumor agents. 256. Conjugation of paclitaxel with other antitumor agents: evaluation of novel conjugates as cytotoxic agents. Research Abstract Details 

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Antitumor agents. 256. Conjugation of paclitaxel with other antitumor agents: evaluation of novel conjugates as cytotoxic agents. Abstract Text:

Kyoko Nakagawa-Goto,Seikou Nakamura,Kenneth F Bastow,Alexander Nyarko,Chieh-Yu Peng,Fang-Yu Lee,Fang-Chen Lee,Kuo-Hsiung Lee,

Sixteen different taxoid conjugates were prepared by linking various anticancer compounds, including camptothecin (CPT), epipodophyllotoxin (EP), colchicine (COL), and glycyrrhetinic acid (GA), at the 2'- or 7-position on paclitaxel (TXL, 1) through an ester, imine, amine, or amide bond. Newly synthesized conjugates were evaluated for cytotoxic activity against replication of several human tumor cell lines. Among them, TXL-CPT conjugates, 8-10, were more potent than TXL itself against the human prostate carcinoma cell line PC-3 (ED(50)=14.8, 3.1, 19.4nM compared with 55.5nM), and conjugate 10 was also 8-fold more active than TXL against the LN-CAP prostate cancer cell line. These compounds also possessed anti-angiogenesis ability as well as lower inhibitory effects against a normal cell line (MRC-5). Thus, conjugates 8-10 are possible antitumor drug candidates, particularly for prostate cancer.

Antitumor agents. 256. Conjugation of paclitaxel with other antitumor agents: evaluation of novel conjugates as cytotoxic agents. Publishing Authors By Initials

K Nakagawa-Goto,S Nakamura,KF Bastow,A Nyarko,CY Peng,FY Lee,FC Lee,KH Lee,

For similar cells: cells, cultured: tumor cells, cultured research abstracts see: cells: cells, cultured: tumor cells, cultured research

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MEDLINE DATE:

Antitumor agents. 256. Conjugation of paclitaxel with other antitumor agents: evaluation of novel conjugates as cytotoxic agents. Journal Published:

PUBLICATION TYPE: Research Support, N.I.H., Extr

Journal: Bioorganic & medicinal chemistry letters

VOLUME: 17

Page Numbers: 2894-8

Journal Abbreviation:

ISSN: 0960-894X

DAY: 27

MONTH: 02

YEAR: 2007

Antitumor agents. 256. Conjugation of paclitaxel with other antitumor agents: evaluation of novel conjugates as cytotoxic agents. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 9107377

Antitumor agents. 256. Conjugation of paclitaxel with other antitumor agents: evaluation of novel conjugates as cytotoxic agents. Keywords Mesh Terms:

KEYWORDS: Tumor Cells, Cultured

MESH TERMS: pharmacology

Chemical & Substance for Abstract: Antitumor agents. 256. Conjugation of paclitaxel with other antitumor agents: evaluation of novel conjugates as cytotoxic agents. Information

Substance Name: Paclitaxel

Registry Number: 33069-62-4

Grant and Affiliation Information for Antitumor agents. 256. Conjugation of paclitaxel with other antitumor agents: evaluation of novel conjugates as cytotoxic agents.

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

Country: England

AGENCY: United States NCI

GRANT: CA-17625

ACRONYM: CA

MEDLINETA: Bioorg Med Chem Lett

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