期刊
CHEMICAL & PHARMACEUTICAL BULLETIN
卷 65, 期 10, 页码 973-981出版社
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.c17-00409
关键词
pyrrolo[2,1-a]isoquinoline; synthesis; cytotoxic activity
资金
- Conacyt (Consejo Nacional de Ciencia y Tecnologia) [131295, 223141]
- Direccion General de Asuntos del Personal Academic (DGAPA), Universidad Nacional Autonoma de Mexico (UNAM) [PAPIIT IN213407]
- Conacyt Graduate Scholarship [223441]
In this study, therpyrrolo[2,1-a]isoquinolines 4a-n were synthesized in good yields in a three steps synthesis from the corresponding a,beta-unsaturated esters starting materials. These compounds were tested on six human cancer cells lines to measure the cytotoxic activity as a function of the electronic properties and aromaticity of the substituent at the C-2 position of the pyrroloisoquinoline. Our results reveal that the cytotoxic activity could be explained in terms of the distribution of electronic density across the ring joined to C-2. Also, this study identified 3-hydroxy (4d) and 3-chloro (4j) derivatives with powerful cytotoxic activities. The IC50 values of these compounds were found to be comparable to those of the commercially available Topotecan, Irinotecan, Etoposide, Tamoxifen, and Cisplatin.
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