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

Boqiao Fu; Yingjie Li; Shaoyong Peng; Xiaolin Wang; Jingying Hu; Long Lv; Caifen Xia; Dai Lu; Caiqin Qin

doi:10.1098/rsos.201642

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

R Soc Open Sci. 2021 Feb 24;8(2):201642. doi: 10.1098/rsos.201642.

Authors

Boqiao Fu¹, Yingjie Li², Shaoyong Peng², Xiaolin Wang², Jingying Hu³, Long Lv¹, Caifen Xia¹, Dai Lu⁴, Caiqin Qin¹

Affiliations

¹ Hubei Provincial Collaborative Innovation Center of Biomass Resources Transformation and Utilization, College of Chemistry and Materials Science, Hubei Engineering University, Hubei 432000, People's Republic of China.
² Guangdong Institute of Gastroenterology, Guangdong Provincial Key Laboratory of Colorectal and Pelvic Floor Diseases, The Sixth Affiliated Hospital, Sun Yat-sen University, Guangzhou, Guangdong 510655, People's Republic of China.
³ State Key Laboratory of Oncogenes and Related Genes, Shanghai Cancer Institute, Renji Hospital, Shanghai Jiaotong University School of Medicine, Shanghai 200032, People's Republic of China.
⁴ Department of Pharmaceutical Sciences, Rangel College of Pharmacy, Texas A&M University, TX 78363, USA.

Abstract

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.

Keywords: 293T; HCT-116; colon cancer; glucopyanosyl-conjugated benzyl.

Associated data

figshare/10.6084/m9.figshare.c.5305520