• Archives of Pharmacal Research
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• v.20 no.3
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• pp.264-268
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• 1997

In order to study the structure-activity relationship of 7, 8-dimethoxy-2-methyl-3-(4, 5-methylenedioxy-2-vinylphenyl)isoquinoline-1(2H) -one (2), which has exhibited significant antitumor activity, chemical modifications of 2 were performed to yield the corresponding products (3-7). Further systematic uses of an efficient procedure for the synthesis of 3-arylisoquinoline derivatives produced the substituted compounds (9a-9g), which were tested for in vitro antitumor activity against five different human cancer cell lines.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.340.3-341
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• 2002

During the research for the development of antitumor agents. we found the 3-arylisoquinoline derivatives exhibited potent cytotoxicity against human tumor cell lines. For extending our study on these compounds. indeno［1.2-c］isoquinolines were chosen as the next research target due to previous studied data of the compounds that showed potent topoisomerase I inhibition activity as well as cytotoxicity against many kinds of tumor cell lines. Retrosynthetic consideration of indeno[1.2-d]isoquinolines indicates that the coupling of o-methyltoluamide with o-hydroxymethylbenxonitrile might afford 3-arylisoquinoline which could be translerred to the aldehtde. Indeno [1.2-c]isoquinolines can be formed by and inframolecular ring cyclization method. Various derlvatives of this compound including 11-alkoxy-6-methyl-6H. 11H-indeno[1.2-c]isoquinolin-5-one and biological activity will be presented with the docking model with topisomerase 1 enzyme.

• YAKHAK HOEJI
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• v.46 no.4
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• pp.219-225
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• 2002

We have performed a 3D-QSAR/CoMFA analysis of the cytotoxic activities of thirty-five 3-arylisoquinoline derivatives against SK-OV-3 tumor cell line. The results suggested that the electrostatic, steric and hydrophobic factors of 3-arylisoquinolines were strongly correlated with the antitumor activity. Considerable predictive ability (cross-validated r2 as high as 0.841) was obtained through CoMFA.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.348.2-348.2
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• 2002

The significant antitumor activities of 3-arylisoquinolines promoted us to explore the structure-activity relationship of these compounds. A series of 3-Arylisoquinoline derivatives, which related to Benzo［c］ phenanthridine alkaloids. were evaluated for antitumor cytotoxicity against human lung tumor cell (A 549). We tried to study structure-activity relationship (SAR) of 3-Arylisoquinolines using the comparative molecular field analysis (CoMFA) method. (omitted)

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.171.1-171.1
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• 2003

·The potent antitumor activities of 3-arylisoquinolines promoted us to explore the structure-activity relationship of these compounds. A series of 3-arylisoquinoline derivatives were evaluated for antitumor cytotoxicity against human lung tumor cell (A 549). For the next stage, we decided to prepare the constrained form of 3-arylisoquinolines as indeno[1,2-c]isoquinolines. As a result, diverse spectrum against human tumor cell lines was obtained. In order to study structure-activity relationship (SAT) of these compounds the comparative molecular field analysis (CoMFA) was carried out. (omitted)