Novel Carborane Compounds Based on Cyclooxygenase‐2 Inhibitors for Effective Boron Neutron Capture Therapy of Tongue Squamous Cell Carcinoma. Issue 46 (8th December 2020)

• Record Type: Journal Article
• Authors: Zhang, Taofeng; Du, Shaobo; Wang, Yu; Guo, Yanzhu; Yi, Yangman; Liu, Bin; Liu, Yang; Chen, Ximeng; Zhao, Quanyi; He, Dian; Wang, Zhen; Zhang, Hong; Ma, Qianlong
• Is Part Of: ChemistrySelect. Volume 5:Issue 46(2020)
• Page Start: 14652
• Page End: 14660
• Publication Date: 2020-12-08
• Subjects: Boron neutron capture therapy -- Tongue squamous cell carcinoma -- COX-2 inhibitors -- Biological activity -- Growth factors; Chemistry -- Periodicals; 540.5
• DOI: 10.1002/slct.202004077
• Languages: English
• ISSNs: 2365-6549

Abstract

Abstract: To date, the mortality of tongue squamous cell carcinoma (TSCC) is still high, COX‐2 is highly expressed in the head and neck cancers, and targeting COX‐2 is a potential treatment for TSCC. Herein, a series of novel carborane compounds based on COX‐2 inhibitors have been developed for the effective treatment of TSCC by boron neutron capture therapy (BNCT). Notably, the compound 1 had high COX‐2 selectivity and low cytotoxicity against CAL27 cells. Meanwhile, the compound 1 had higher selectivity and uptake of CAL27 cells compared to the positive control group sodium borocaptate (BSH). The apoptosis of CAL27 cells treated with the compound 1 during BNCT was significantly induced by breaking DNA double strands and generating excess reactive oxygen species, and the proliferation of cancer cells was inhibited by down‐regulating the expression of cytokines associated with phosphatidylinositide 3‐kinases/protein kinase B (PI3K/Akt) and mitogen‐activated protein kinases (MAPKs) signaling pathways in BNCT. Thus, the carborane compounds based on COX‐2 inhibitors have the potential to effectively treat tongue squamous cell carcinoma through BNCT. Abstract : Novel carborane compounds based on COX‐2 inhibitors have been developed for the effective treatment of tongue squamous cell carcinoma by boron neutron capture therapy (BNCT). The apoptosis of the compound treated CAL27 cells during BNCT was significantly induced, and the proliferation of cancer cells was inhibited. Overall, the carborane‐containing COX‐2 inhibitors have the potential toeffectivelytreat tongue squamous cell carcinoma through BNCT.