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KMID : 0369919920070000001
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Journal of Pharmaceutical Sciences (C.B.N.)
1992 Volume.7 No. 0 p.1 ~ p.4
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Influence of 2-(sub. phenyl) group on the Cytotoxic Activity of 2-(sub. phenyl)-benzimidazole-4-carboxa mide Derivatives as Potential Antitumor Agents
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Myung, Pyung Keun
Kim, Dong Sun/Lee, Chun Bae/Sung, Nack-Do
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Abstract
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The quantitative structure-activity relationships (QSAR) between antitumor a.ctivity(pICso) against P388/W cell line and the binding constant(log KAT) to polyCd(AT)), and the physicochemical parameters of substituents on the 2-phenyl groups (PBIC) were analyzed by the multiple regression technique. The activity is related parabolically to the STERIMOL parameter (L, & B:,) of the 2-substituted phenyl moieties. When the parasubstituents (RI) on the 2-substituted phenyl group has optimal values (L=10A & B1=2.20A) and minimal value (above ir=0.67^0.82), highly cytotoxic activity in-vitro against P338/W murine leukemia is expected.
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KEYWORD
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