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- W2047430129 abstract "Abstract Colchicine is a cytotoxic bioactive alkaloid that exhibits its action by microtubular binding. With an aim to develop a tumor targeted radio‐therapeutic agent, colchicine has been functionalized to trimethylcolchicinic acid and conjugated to the isothiocyanato derivative of DOTA (1,4,7,10‐tetraaza cyclododecane tetracetic acid). DOTA coupled colchicine was radiolabeled with 90 Y, one of the most commonly used therapeutic radioisotope. Complexation of 200 µg of the conjugate with 90 Y was carried out at pH 4.5 with an incubation time of 45 min at 70°C. Complexation yield of 90 Y‐DOTA‐NCS‐colchicine was confirmed to be >98% using C‐18 reverse phase HPLC system. 90 Y‐colchicine complex could be differentiated from 90 Y‐ p ‐NCS‐benzyl‐DOTA on the basis of difference in their retention times 8 and 4 min, respectively in a standardized HPLC system. Biodistribution studies in Swiss mice fibrosarcoma tumor model showed an uptake of ∼0.8% ID/g tumor at 3 h.p.i. that was retained till 24 h.p.i. 90 Y‐DOTA‐NCS‐colchicine complex showed excellent pharmacokinetics with major portion of the radioactivity being excreted out within 3 h.p.i. and no accumulation of radioactivity in vital organs. Copyright © 2006 John Wiley & Sons, Ltd." @default.
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- W2047430129 date "2006-09-04" @default.
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- W2047430129 title "Synthesis and evaluation of90Y-DOTA-Colchicine conjugate in murine fibrosarcoma model" @default.
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- W2047430129 doi "https://doi.org/10.1002/jlcr.1115" @default.
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