138441-82-4Relevant articles and documents
Antitumor agents. 256. Conjugation of paclitaxel with other antitumor agents: Evaluation of novel conjugates as cytotoxic agents
Nakagawa-Goto, Kyoko,Nakamura, Seikou,Bastow, Kenneth F.,Nyarko, Alexander,Peng, Chieh-Yu,Lee, Fang-Yu,Lee, Fang-Chen,Lee, Kuo-Hsiung
, p. 2894 - 2898 (2008/02/03)
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 (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.
MOLECULAR CONSTRUCTS SUITABLE FOR TARGETED CONJUGATES
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Page/Page column 30-31, (2008/06/13)
The present invention relates generally to effective drug-linker constructs suitable for conjugation with ligands. The present invention also discloses methods of conjugating these constructs with peptides to form the compound of formula I. These methods are readily extended to any hydroxyl, amine or sulfur bearing biologically active molecules.