Affiliation:
1. CAS Key Laboratory of Polymer Ecomaterials Changchun Institute of Applied Chemistry, Chinese Academy of Sciences Changchun P. R. China
2. College of Applied Chemistry and Engineering University of Science and Technology of China Hefei P. R. China
Abstract
AbstractTirapazamine (TPZ, 3‐amino‐1,2,4‐benzotriazine 1,4‐dioxide), a representative hypoxia‐activated prodrugs (HAPs), has entered Phase II/III clinical trials. Despite a promising phase II clinical trial results, TPZ does not bring benefits to cancer therapy in most phase III clinical trials, which making the clinical trials failed. To improve its therapeutic effects, in this study, we synthesize a novel TPZ derivative, 3‐(3‐(5‐hydroxypentyl)ureido)benzo[e][1,2,4]triazine 1,4‐dioxide (TPZH), and covalently conjugated it to poly (L‐glutamic acid) (PLG) to obtain TPZH nanoparticles (TPZH‐NPs). The TPZH‐NPs shows prolonged blood circulation, enhanced tumor accumulation, and increased maximum tolerated dose (MTD) than TPZH. In addition, TPZH‐NPs exhibits significantly enhanced antitumor therapeutic efficiency than free TPZH against 4T1 breast tumors.
Funder
Ministry of Science and Technology of the People's Republic of China
National Natural Science Foundation of China
Youth Innovation Promotion Association of the Chinese Academy of Sciences
Subject
Materials Chemistry,Polymers and Plastics,Physical and Theoretical Chemistry
Cited by
1 articles.
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