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

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dc.contributor.author Nakagawa-Goto, K.
dc.contributor.author Nakamura, S.
dc.contributor.author Bastow, K.F.
dc.contributor.author Nyarko, A. K.
dc.contributor.author Peng, C.Y.
dc.contributor.author Lee, F.Y.
dc.contributor.author Lee, K.H.
dc.date.accessioned 2012-05-03T16:57:23Z
dc.date.accessioned 2017-10-16T13:09:23Z
dc.date.available 2012-05-03T16:57:23Z
dc.date.available 2017-10-16T13:09:23Z
dc.date.issued 2007
dc.identifier.uri http://197.255.68.203/handle/123456789/1035
dc.description.abstract Sixteen different taxoid conjugates were prepared by linking various anticancer compounds, including camptothecin (CPT), epipodophyllotoxin (EP), colchicine (COL), and glycyrrhetinic acid (GA), at the 20- 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 (ED50 = 14.8, 3.1, 19.4 nM compared with 55.5 nM), 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. en_US
dc.language.iso en en_US
dc.publisher Bioorganic and Medical Chemistry Letter (17): 2894-8 en_US
dc.subject Paclitaxel en_US
dc.subject Conjugation en_US
dc.subject Cytotoxicity en_US
dc.subject Prostate cancer en_US
dc.title Antitumor agents. 256. Conjugation of paclitaxel with other antitumor agents: evaluation of novel conjugates as cytotoxic agents en_US
dc.type Article en_US


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  • Clinical Pathology Department [56]
    The Clinical Pathology Department conducts research that contributes to intervention strategies and safeguards of public health in Ghana. In view of this the Department carries out research into plant medicine development, drug interactions and regulation, bio-monitoring and prevention of poisoning from environmental toxicants (e.g. mycotoxins specifically aflatoxins and toxic heavy metals). The Department also provides specialized laboratory services in support of public health programmes.

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