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. 2017 Jun 15;27(12):2793-2799.
doi: 10.1016/j.bmcl.2017.04.070. Epub 2017 Apr 22.

Cell line studies and analytical measurements of three paclitaxel complex variations

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Cell line studies and analytical measurements of three paclitaxel complex variations

Thomas Manning et al. Bioorg Med Chem Lett. .

Abstract

The copper(II) cation, sucrose, and hydroxychloroquine were complexed with the chemotherapy agent paclitaxel and studied for medicinal activity. Data (GI50, LD50) from single dose and five dose National Cancer Institute sixty cell line panels are presented. Analytical measurements of different complexes were made using Nuclear Magnetic Resonance (1H NMR), Matrix Assisted Laser Desorption Ionization-Time of Flight-Mass Spectrometry (MALDI-TOF-MS) and Fourier Transform-Ion Cyclotron Resonance (FT-ICR). Molecular modeling is utilized to better understand the impact that species could have on physical parameters associated with Lipinski's Rule of Five, such as logP and TPSA. On average, Cu(II) and hydroxychloroquine decreased GI50 values, while sucrose increased GI50 values of paclitaxel.

Keywords: Cancer; Cell line; Copper; Hydroxychloroquine; Paclitaxel; Sucrose.

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