4.6 Article

Synthesis and pharmacological characterization of glucopyranosyl-conjugated benzyl derivatives as novel selective cytotoxic agents against colon cancer

Journal

ROYAL SOCIETY OPEN SCIENCE
Volume 8, Issue 2, Pages -

Publisher

ROYAL SOC
DOI: 10.1098/rsos.201642

Keywords

glucopyanosyl-conjugated benzyl; colon cancer; HCT-116; 293T

Funding

  1. Natural Science Foundation of Xiaogan, China [XGKJ2019010046]
  2. Hubei University Excellent Young and Middle-Aged Science and Technology Innovation Team Project [T201816]
  3. Natural Science Foundation of Hubei Province, China [2014CFB570]
  4. National Natural Science Foundation of China [21503075, 81502022]
  5. Fundamental Research Fund for the Sun Yat-sen University [16ykpy35]

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A new glucopyranosyl-conjugated benzyl derivative containing a [1,2,3]-triazole linker was synthesized and showed potent antiproliferative activity against colorectal cancer cells, inducing apoptotic cell death.
Glucopyranosyl-conjugated benzyl derivatives containing a [1,2,3]-triazole linker were synthesized. Benzyl served as an important pharmacophore in anti-cancer compounds. Compound 8d inhibited the proliferation of colorectal cancer cells with the potency comparable to 5-fluorouracil (5-FU) with improved selectivity towards cancer cells. The antiproliferative activity of 8d is achieved through triggering apoptotic cell death.

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