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|Title:||Design, synthesis and characterisation of a novel anticancer prodrug having antiproliferative activity against prostrate tumour|
|Series/Report no.:||<b>Int</b>.<b>Cl</b>.<b><sup>7</sup> C 07 C</b>|
|Abstract:||A curcumin glycine conjugate viz. 1,7-bis (4<i>-O-</i>glycinoyl-3-methoxyphenyl)-1,6-heptadiene- 3, 5 dione <b>1</b> previously shown by this lab to be having antioxidant, antibacterial and antifungal activity is synthesized and after attachment of a linker (-CH<sub>2</sub>-CH<sub>2</sub>-OH) <b>2</b> is phosphitylated. The phosphitylated unit <b>3</b> was covalently linked to 5´-GT TAG GGT TAG-3´ <b>4</b>, a complementary sequence of 5´-CU AAC CCU AAC-3´, which is the repeat sequence of telomerase RNA template. The comparative melting temperatures (<i>Tm</i>) of modified and normal duplexes have indicated more thermal stability of duplex with bioconjugate. The biodegradable nature of the covalent bond of the prodrug has now been proved by carrying out enzymatic digestion studies. The prostrate tumour derived DU145 cells are transfected with 5´-<i>O-</i>curcumin DNA and study of antiproliferative activity indicated 80% reduction in cell proliferation by the end of 75 days.|
|Appears in Collections:||IJC-B Vol.44B(12) December 2005]|
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