Syntheses, antitumor activities, and antiangiogenesis of a monomer and its medium molecular weight polymers: Maleimidoethanoyl-5-fluorouracil and its polymers

Jung, Eun‐Young; Chung, Ildoo; Lee, Neung-Ju; Park, Jang-Su; Ha, Chang‐Sik; Cho, Won‐Jei

doi:10.1002/(sici)1099-0518(20000415)38:8<1247::aid-pola8>3.3.co;2-6

Cited by 8 publications

(15 citation statements)

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“…Ottenbrite et al 13 reported that medium molecular weight polymers of 10 000–30 000 play a significant role in biological activity. Therefore, we controlled the molecular weights of the polymers by using the photopolymerization method on the basis of our previous studies,18–21 and the molecular weights of the polymers obtained were in a reasonable range to exhibit antitumour activity.…”

Section: Resultsmentioning

confidence: 99%

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Synthesis and biological activity of medium molecular weight polymers containing 3,6-endo-methylene-1,2,3,6-tetrahydrophthalimidobutanoyl-5-fluorouracil

et al. 2000

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Section: Resultsmentioning

confidence: 99%

“…Many attempts have been made to obtain polymers having both higher antitumour activity and lower toxic side‐effects 7–16. We have already reported the synthesis and biological activity of polymers containing 5‐FU 17–21…”

Section: Introductionmentioning

confidence: 99%

Synthesis and biological activity of medium molecular weight polymers containing 3,6-endo-methylene-1,2,3,6-tetrahydrophthalimidobutanoyl-5-fluorouracil

et al. 2000

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“…Radiochemical purity of the complex was determined by chromatographic techniques. The overall labeling yield of the 99m Tc‐5‐FU complex was calculated to be more than 98.1 ± 1.2% . Furthermore, Young et al used simple basic radiochemical reactions for the radiolabeling of the 5‐FU.…”

Section: Discussionmentioning

confidence: 99%

“…5‐Fluorouracil (5‐FU) is an effective antitumor drug, which has been used either as a single agent or in combination with other chemotherapeutic agents for the treatment of tumors such as breast and colorectal carcinoma . 5‐FU is an antimetabolite drug and works by inhibiting essential biosynthetic processes or by being incorporated into macromolecules, such as DNA and RNA.…”

Section: Introductionmentioning

confidence: 99%

Radiolabeling and in vitro evaluation of a new 5‐fluorouracil derivative with cell culture studies

İlem-Özdemir

Gündoğdu

Ekinci

et al. 2019

Labelled Comp Radiopharmac

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The clinical impact and accessibility of 99mTc tracers for cancer diagnosis would be greatly enhanced by the availability of a new, simple, and easy labeling process and radiopharmaceuticals. 5‐Fluorouracil is an antitumor drug, which has played an important role for the treatment of breast carcinoma. In the present study, a new derivative of 5‐Fluorouracil was synthesized as (1‐[{1′‐(1′′‐deoxy‐2′′,3′′:4′′,5′′‐di‐O‐isopropylidene‐β‐D‐fructopyranose‐1′′‐yl)‐1′H‐1′,2′, 3′‐triazol‐4′‐yl}methyl]‐5‐fluorouracil) (E) and radiolabeled with 99mTc. It was analyzed by radio thin layer chromatography for quality control and stability. The radiolabeled complex was subjected to in vitro cell‐binding studies to determine healthy and cancer cell affinity using HaCaT and MCF‐7 cells, respectively. In addition, in vitro cytotoxicity studies of compound E were performed with HaCaT and MCF‐5 cells. The radiochemical purity of the [99mTc]TcE was found to be higher than 90% at room temperature up to 6 hours. The radiolabeled complex showed higher specific binding to MCF‐7 cells than HaCaT cells. IC50 values of E were found 31.5 ± 3.4 μM and 20.7 ± 2.77 μM for MCF‐7 and HaCaT cells, respectively. The results demonstrated the potential of a new radiolabeled E with 99mTc has selective for breast cancer cells.

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“…5 Subsequently, many attempts were made to reduce the toxic side‐effects 6–12. We also have reported the syntheses and biological activities of polymeric antitumour agents such as 5‐fluorouracil (5‐FU) containing acryl derivative polymers,13–18 tetrahydrophthalic acid derivative polymers,19–24 poly(diallyl ether‐ co ‐maleic anhydride),25 poly(glycinyl maleic acid) derivatives,26, 27 and methoxyitaconyl‐5‐fluorouracil,28 and discussed their reduced toxicity and improved antitumour activity.…”

Section: Introductionmentioning

confidence: 99%

Syntheses, antitumour activities and antiangiogenesis of 1,2,3‐tris(ethoxycarbonyl)‐2‐propyl acrylate and its polymers

Kim

Chung

Lee

et al. 2001

Polymer International

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A new monomer, 1,2,3‐tris(ethoxycarbonyl)‐2‐propyl acrylate (TPA), was synthesized by reaction of acryloyl chloride and triethyl citrate. The homopolymer of TPA and its copolymers with acrylic acid (AA), vinyl acetate (VAc) and maleic anhydride (MAH) were prepared by polymerization using lauroyl peroxide (LPO) at 70 °C for 24 h. The structures of TPA and its polymers were identified by FTIR, 1H NMR, 13C NMR spectroscopies, and elemental analysis. The number average molecular weights and polydispersity indices of the synthesized polymers determined by GPC were in the range 4200–23 000 g mol−1 and 1.1–2.1, respectively. The IC50 values of the synthesized samples against cancer cell lines were greater than those of 5‐fluorouracil (5‐FU). The percentage inhibition values of SV40 DNA replication were 82.2 for TPA, 34.3 for poly (TPA), 81.9 for poly(TPA‐co‐AA), 82.0 for poly(TPA‐co‐VAc), 35.6 for poly(TPA‐co‐MAH) and 12.7 for 5‐FU. The inhibitions of SV40 DNA replication and antiangiogenesis for the synthesized TPA and its polymers are much greater than those of the control. © 2001 Society of Chemical Industry

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Syntheses, antitumor activities, and antiangiogenesis of a monomer and its medium molecular weight polymers: Maleimidoethanoyl-5-fluorouracil and its polymers

Cited by 8 publications

References 0 publications

Synthesis and biological activity of medium molecular weight polymers containing 3,6-endo-methylene-1,2,3,6-tetrahydrophthalimidobutanoyl-5-fluorouracil

Synthesis and biological activity of medium molecular weight polymers containing 3,6-endo-methylene-1,2,3,6-tetrahydrophthalimidobutanoyl-5-fluorouracil

Radiolabeling and in vitro evaluation of a new 5‐fluorouracil derivative with cell culture studies

Syntheses, antitumour activities and antiangiogenesis of 1,2,3‐tris(ethoxycarbonyl)‐2‐propyl acrylate and its polymers

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