Synthesis of 1-benzyl-3-(5-hydroxymethyl-2-furyl)selenolo[3,2- c]pyrazole derivatives as new anticancer agents

As part of our continuing search for potential anticancer drug candidates among YC-1 analogs, 1, 3-disubstituted selenolo[3,2- c]pyrazole derivatives were synthesized and evaluated for their cytotoxicity against NCI-H226 non-small cell lung cancer and A-498 renal cancer cell lines. Significant cytot...

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Published in:European journal of medicinal chemistry 2010-04, Vol.45 (4), p.1395-1402
Main Authors: Chou, Li-Chen, Huang, Li-Jiau, Hsu, Mei-Hua, Fang, Mei-Chi, Yang, Jai-Sing, Zhuang, Shi-Hong, Lin, Hui-Yi, Lee, Fang-Yu, Teng, Che-Ming, Kuo, Sheng-Chu
Format: Article
Language:English
Subjects:
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Biological and medical sciences
Cell Line, Tumor
Cytotoxicity
Drug Screening Assays, Antitumor
Furopyrazole
General aspects
Humans
Magnetic Resonance Spectroscopy
Medical sciences
Pharmacology. Drug treatments
Pyrazoles - chemical synthesis
Pyrazoles - chemistry
Pyrazoles - pharmacology
Selenolopyrazole
Spectrophotometry, Infrared
Structure–activity relationships (SAR)
Thienopyrazole
YC-1 analogs
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Summary:As part of our continuing search for potential anticancer drug candidates among YC-1 analogs, 1, 3-disubstituted selenolo[3,2- c]pyrazole derivatives were synthesized and evaluated for their cytotoxicity against NCI-H226 non-small cell lung cancer and A-498 renal cancer cell lines. Significant cytotoxicity was observed in 3-(5-hydroxymethyl-2-furyl) derivatives ( 2, 33, 36 and 37). Among them, compound 2 was found to have the most potent activity. The mode of action of compound 2 seems to differ from those of the 175 anticancer agents listed in NCI's standard database and resembles that of YC-1. Thus, we recommend that compound 2 should be developed further as new drug candidate for treatment of non-small cell lung cancer and renal cancer. [Display omitted]
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2009.12.039