Preclinical antitumor efficacy of analogs of XK469: sodium-(2-[4-(7-chloro-2-quinoxalinyloxy)phenoxy]propionate

Add time:09/30/2019    Source:infona.pl

A series of quinoxaline analogs of the herbicide Assure® was found to have selective cytotoxicity for solid tumors of mice in a disk-diffusion-soft-agar-colony-formation-assay compared to L1210 leukemia. Four agents without selective cytotoxicity and 14 agents with selective cytotoxicity were evaluated in vivo for activity against a solid tumor. The four agents without selective cytotoxicity in the disk-assay were inactive in vivo (T/C > 42%). Thirteen of the fourteen agents with selectivity in the disk-assay were active in vivo (T/C < 42%). Five of the agents had curative activity. These five agents had a halogen (F, Cl, Br) in the 7-position (whereas Assure® had a Cl in the 6 position). All agents with curative activity were either a carboxylic acid, or a derivative thereof, whereas Assure® is the ethyl ester of the carboxylic acid. All other structural features were identical between Assure® and the curative agents. Assure® had no selective cytotoxicity for solid tumors in the disk-assay, and was devoid of antitumor activity. The analog XK469 is in clinical development.

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Prev:Linkage of boronated polylysine to glycoside moieties of polyclonal antibody; boronated antibodies as potential delivery agents for neutron capture therapy1 1Abbreviations: BNCT, Boron neutron capture therapy; BPL, Boronated poly-DL-lysine; BSA, Bovine serum albumin; DMBA, p-Dimethylaminobenzaldehyde; DMF, Dimethylformamide; DMSO, Dimethyl sulfoxide; DTT, Dithiothreitol; FTSC, Fluorescein thiosemicarbazide; HRP, Horseradish peroxidase; IgG, Immunoglobulin-G; IRMA, Immunoradiometric assay; LET, Linear energy transfer; MB-hydrazide, m-Maleimidobenzoyl hydrazide; MW, Molecular weight; PBS, Phosphate buffered saline; PL, Poly-DL-lysine; SDS-PAGE, Sodium n-Dodecyl Sulfate Polyacrylamide Gel Electrophoresis; SPDP, N-Succinimidyl-3-(2 pyridyldithio) propionate; Sulfo-MBS, m-Maleimidobenzoyl-N-hydroxysulfosuccinimide ester; TRIZMA®, Tris (hydroxymethyl) aminomethane; TSH, Thyroid stimulating hormone.
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