Potential Anti-Tumor Drug: Co-Crystal 5-Fluorouracil-nicotinamide

Zhuyan Zhang; Nan Yu; Chang Xue; Shan Gao; Zhaopeng Deng; Min Li; Cong Liu; John Castellot; Siying Han

doi:10.1021/acsomega.9b03574

Potential Anti-Tumor Drug: Co-Crystal 5-Fluorouracil-nicotinamide

ACS Omega. 2020 Jun 24;5(26):15777-15782. doi: 10.1021/acsomega.9b03574. eCollection 2020 Jul 7.

Authors

Zhuyan Zhang^{1

2}, Nan Yu¹, Chang Xue³, Shan Gao², Zhaopeng Deng², Min Li¹, Cong Liu⁴, John Castellot⁵, Siying Han⁴

Affiliations

¹ Pharmaceutical Experiment Teaching Center, College of Pharmacy, Harbin Medical University, Harbin 150081, China.
² Key Laboratory of Functional Inorganic Material Chemistry, Ministry of Education, School of Chemistry and Materials Science, Heilongjiang University, Harbin 150080, China.
³ Tufts University Sackler School of Biomedical Sciences, Boston, Massachusetts 02111, United States.
⁴ Department of Pharmaceutical Analysis and Analytical Chemistry, College of Pharmacy, Harbin Medical University, Harbin 150081, China.
⁵ Department of Integrative Physiology and Pathobiology, Tufts University School of Medicine, Boston, Massachusetts 02111, United States.

Abstract

5-Fluorouracil-nicotinamide (5-FU-NCM), a co-crystal with a 2D layer structure formed by hydrogen bonds, was synthesized by solvent evaporation and liquid phase-assisted grinding at room temperature. Compared to 5-FU alone, the results of solubility, oil-water partition coefficient, anti-tumor effect in vivo and vitro, acute toxicity, and pharmacokinetic parameters indicate that the co-crystal is a potential anti-tumor drug.