Literature

Abstract

A novel series of maleamic amino acid ester conjugates of 3,5-bisarylmethylene-4-piperidones were prepared to investigate the efficacy of micronutrient conjugation in enhancing cytotoxic potency by improving selectivity and delivery. These compounds, prepared as anticancer agents, were expected to demonstrate enhanced selectivity towards malignant cells through the inhibition of topoisomerase IIalpha via protein thiolation. The cytostatic effects of these compounds were evaluated against three cell lines, namely murine L1210 leukemia cells, human Molt 4/C8 and CEM T-lymphocyte cells. All compounds were found to have greater potency than the reference drug melphalan. Several compounds were found to potently inhibit topoisomerase IIalpha and displayed cytostatic activity in the nanomolar range.

DOI： 10.1016/j.bmcl.2009.09.069

Design, synthesis and bioevaluation of novel maleamic amino acid ester conjugates of 3,5-bisarylmethylene-4-piperidones as cytostatic agents

Bioorganic & Medicinal Chemistry Letters 2009.0

Investigation of fatty acid conjugates of 3,5-bisarylmethylene-4-piperidone derivatives as antitumor agents and human topoisomerase-IIα inhibitors

Bioorganic & Medicinal Chemistry 2015.0

Indeno[1,2-c]isoquinolin-5,11-diones conjugated to amino acids: Synthesis, cytotoxicity, DNA interaction, and topoisomerase II inhibition properties

Bioorganic & Medicinal Chemistry 2010.0

Imine/amide–imidazole conjugates derived from 5-amino-4-cyano- N 1-substituted benzyl imidazole: Microwave-assisted synthesis and anticancer activity via selective topoisomerase-II-α inhibition

Bioorganic & Medicinal Chemistry 2015.0

Synthesis and biological evaluation of N -(carbobenzyloxy)- l -phenylalanine and N -(carbobenzyloxy)- l -aspartic acid- β -benzyl ester derivatives as potent topoisomerase IIα inhibitors

Bioorganic & Medicinal Chemistry 2017.0

Tumour-specific cytotoxicity and structure–activity relationships of novel 1-[3-(2-methoxyethylthio)propionyl]-3,5-bis(benzylidene)-4-piperidones