A comparative study of antitumour and toxicologic properties of related polyanions

Ottenbrite, Raphael M.; Goodell, Estelle M.; Munson, Albert E.

doi:10.1016/0032-3861(77)90162-8

Cited by 27 publications

(4 citation statements)

References 12 publications

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“…The early development of DIVEMA has inspired testing of anticancer activity of variety of synthetic polymers, including poly(maleic anhydride), poly(acrylic acid–maleic anhydride) copolymers [15], poly(acrylic acid), poly(vinyl sulfate), and poly(amido amine)s [16,17]. Many of these polymers exhibited significant antitumor activity and prolonged survival in animal models either by direct toxicity to tumor cells or indirectly by activation of the immune system.…”

Section: Polymeric Drugs In Cancer Treatmentmentioning

confidence: 99%

Polymeric drugs: Advances in the development of pharmacologically active polymers

Jing

Chen

et al. 2015

Journal of Controlled Release

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Synthetic polymers play a critical role in pharmaceutical discovery and development. Current research and applications of pharmaceutical polymers are mainly focused on their functions as excipients and inert carriers of other pharmacologically active agents. This review article surveys recent advances in alternative pharmaceutical use of polymers as pharmacologically active agents known as polymeric drugs. Emphasis is placed on the benefits of polymeric drugs that are associated with their macromolecular character and their ability to explore biologically relevant multivalency processes. We discuss the main therapeutic uses of polymeric drugs as sequestrants, antimicrobials, antivirals, and anticancer and anti-inflammatory agents.

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Section: Polymeric Drugs In Cancer Treatmentmentioning

confidence: 99%

Polymeric drugs: Advances in the development of pharmacologically active polymers

Jing

Chen

et al. 2015

Journal of Controlled Release

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“…Our preliminary data [12] showed that benzocaine conjugated to an anionic polymer system can reduce side effects while maintaining or even increasing the antitumor effect of the test drug. Benzocaine (ethyl p-aminobenzoate) is used topically for the temporary relief of pain and itching associated with minor burns, sunburn, minor cuts or scrapes, insect bites, or minor skin irritations.…”

Section: Introductionmentioning

confidence: 96%

“…This pyran as well as specific molecular weight fractions of MVE (1-6) have been investigated extensively from the standpoint of both its chemical structure and its antitumor activity [7][8][9][10][11]. Based on the structural studies of DIVEMA, a large number of additional copolymers based on maleic anhydride were synthesized and characterized [12][13][14][15][16][17][18]. Many of these copolymers were evaluated for their antitumor properties by the NIH.…”

Section: Introductionmentioning

confidence: 99%

Biological Effects and Antitumor Activity Induced by Benzocaine Conjugated Anionic Polymers

Panaitescu

Ottenbrite

2002

Journal of Bioactive and Compatible Polymers

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Three maleic anhydride copolymers [poly(maleic anhydride-vinyl acetate), poly(maleic anhydride-styrene) and poly(maleic anhydride-methyl methacrylate)] were prepared as well as the corresponding benzocaine conjugates. The maleic anhydride moiety was hydrolyzed to the corresponding polycarboxylate anions and then biologically evaluated using pyran copolymer as the standard. All of the polymers showed internal organ toxicity of the liver, kidneys and spleen which increased with increasing molecular weight, however, the benzocaine derivatives decreased this effect in most cases. The biological evaluations included hemoglobin levels, hematocrit levels, red blood indices and mean cell volumes which were increased on an average of 50%. The blood protein profiles were not changes significantly; on average they were changed about AE50%. The unmodified copolymers decreased the major serum and cholesterol levels by $75%. The copolymers (with or without) benzocaine decreased both the blood sugar and enzyme profiles. The antitumour activity was evaluated against Walker carcinosarconoma; although the benzocaine enhanced these effects, only pyran and the 18,000 Mw benzocaine-modified poly(maleic anhydride-vinyl acetate) produced significant effects.

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“…Nonetheless, despite its rich pharmacological profile, DIVEMA was also shown to have significant side effects such as pyrogenicity, thrombocytopenia, inhibition of microsomal enzymes, sensitization to endotoxin, liver damage, organomegaly and depression of the reticuloendothelial system. Following initial studies, several attempts have been made to narrow the molecular weight distribution of DIVEMA, thereby minimizing its side effects and optimizing its pharmacological properties 4–10…”

Section: Introductionmentioning

confidence: 99%

Synthesis and biological activity of medium range molecular weight polymers containing exo‐3,6‐epoxy‐1,2,3,6‐tetrahydrophthalimidocaproic acid

Lee

Kang

Cho

et al. 2001

Polymer International

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A new monomer, exo-3,6-epoxy-1,2,3,6-tetrahydrophthalimidocaproic acid (ETCA), was prepared by reaction of maleimidocaproic acid and furan. The homopolymer of ETCA and its copolymers with acrylic acid (AA) or with vinyl acetate (VAc) were obtained by photopolymerizations using 2,2-dimethoxy-2-phenylacetophenone as an initiator at 25°C. The synthesized ETCA and its polymers were identi®ed by FTIR, 1 H NMR and 13 C NMR spectroscopies. The apparent average molecular weights and polydispersity indices determined by gel permeation chromatography (GPC) were as follows: M n = 9600 g mol À1 , M w = 9800 g mol À1 , M w /M n = 1.1 for poly(ETCA); M n = 14 300 g mol À1 , M w = 16 200 g mol À1 , M w /M n = 1.2 for poly(ETCA-co-AA); M n = 17 900 g mol À1 , M w = 18 300 g mol À1 , M w /M n = 1.1 for poly(ETCA-co-VAc). The in vitro cytotoxicity of the synthesized compounds against mouse mammary carcinoma and human histiocytic lymphoma cancer cell lines decreased in the following order: 5-¯uorouracil (5-FU) ! ETCA > polymers. The in vivo antitumour activity of the polymers against Balb/C mice bearing sarcoma 180 tumour cells was greater than that of 5-FU at all doses tested.

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A comparative study of antitumour and toxicologic properties of related polyanions

Cited by 27 publications

References 12 publications

Polymeric drugs: Advances in the development of pharmacologically active polymers

Polymeric drugs: Advances in the development of pharmacologically active polymers

Biological Effects and Antitumor Activity Induced by Benzocaine Conjugated Anionic Polymers

Synthesis and biological activity of medium range molecular weight polymers containing exo‐3,6‐epoxy‐1,2,3,6‐tetrahydrophthalimidocaproic acid

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