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Cyanine-Gemcitabine Conjugates as Targeted Theranostic Agents for Glioblastoma Tumor Cells.

ABSTRACT: A small subset of heptamethine dyes (cyanine-7 or Cy7) share an intriguing characteristic: preferential tumor accumulation and retention. These dyes absorb in the near-infrared (NIR) region (above 750 nm) and perform active targeting to deliver therapeutic and toxic cargoes to various tumor models in vivo. In this work, four heptamethines 1 were synthesized, which have a gemcitabine fragment attached to the meso-position of the Cy7 core. Theranostic agent 1a was discovered that localized in glioblastoma tumor cells, has absorption maxima in NIR region, and showed similar therapeutic effect to gemcitabine but at one-third the molar dose.

SUBMITTER: Jiang Z

PROVIDER: S-EPMC7050787 | biostudies-literature | 2019 Oct

REPOSITORIES: biostudies-literature

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Cyanine-Gemcitabine Conjugates as Targeted Theranostic Agents for Glioblastoma Tumor Cells.

Jiang Zhengyang Z Pflug Kathryn K Usama Syed Muhammad SM Kuai Dacheng D Yan Xin X Sitcheran Raquel R Burgess Kevin K

Journal of medicinal chemistry 20191011 20

A small subset of heptamethine dyes (cyanine-7 or Cy7) share an intriguing characteristic: preferential tumor accumulation and retention. These dyes absorb in the near-infrared (NIR) region (above 750 nm) and perform active targeting to deliver therapeutic and toxic cargoes to various tumor models in vivo. In this work, four heptamethines 1 were synthesized, which have a gemcitabine fragment attached to the meso-position of the Cy7 core. Theranostic agent 1a was discovered t ...[more]

PMID: 31469566

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