Abstract

RN1, a polysaccharide from flowers of Panax pseudo-ginsieng Wall. Var. notoginseng (Burkill) Hoo & Tseng, is a potential multi-targeting drug candidate for pancreatic cancer treatment. However, the active targeting domain of RN1 is still unknown. Herein, three RN1 derived branches were synthesized via [3+2] or [2+2] strategies, efficiently. Two pentasaccharides, 18 and 27, showed similar inhibition effect on pancreatic cancer BxPC-3 cells to that of RN1 at same concentration. Interestingly, tetrasaccharide 21 potently inhibited gemcitabineresistant cell line Panc-1 at high concentration. These suggest that the branches of RN1 might be the active targeting domain and tetrasaccharide 21 might be a potential leading compound for pancreatic cancer with gemcitabine resistance.

Highlights

  • Pancreatic cancer is a cancer with high mortality, which is close to incidence [1]

  • RN1 were of the two possible arabinogalactan branches; (b) Three branches derived from RN1 were synthesized synthesized in this paper

  • We had synthesized three branches derived from RN1 polysaccharide via [3+2] and [2+2]

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Summary

A Concise Synthesis of Three Branches Derived from

Deqin Cai 1,2 , Yanli Yao 1,2 , Yubo Tang 3,4 , Zheng Wang 2,5 , Wei Shi 1,3 , Wei Huang 1,3 and Kan Ding 1,2, *. Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China. Nano Science and Technology Institute, University of Science and Technology of China, 96 Jin Zhai Road, Hefei 230026, China. Received: 8 September 2017; Accepted: 18 October 2017; Published: 21 October 2017

Introduction
General Experimental Procedures
Cells and Materials
Cell Viability Assessment
Retrosynthetic Analysis
Retrosynthetic
The free hydroxyl 8ofwas disaccharide
Exploration of the Synthesis of the Gal-Containing Trisaccharide Donor
Synthesis
Synthesis of the Target and Challenging 27
Anti-Pancreatic Cancer Activity Test
Conclusions
Full Text
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