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.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Animals
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / metabolism
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Antineoplastic Agents / pharmacology
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Antineoplastic Agents / therapeutic use
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Carbocyanines / chemistry*
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Cell Line, Tumor
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Cell Survival / drug effects
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Deoxycytidine / analogs & derivatives*
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Deoxycytidine / chemistry
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Drug Stability
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Female
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Gemcitabine
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Glioblastoma / drug therapy
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Glioblastoma / pathology
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Humans
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Mice
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Mice, Nude
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Theranostic Nanomedicine*
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Tissue Distribution
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Transplantation, Heterologous
Substances
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Antineoplastic Agents
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Carbocyanines
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Deoxycytidine
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Gemcitabine