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Quantitative Structure–Activity Relationship Analysis of Combretastatins: A Class of Novel Antimitotic Agents

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Abstract

Combretastatins and their synthetic analogues, having structural features resembling that of colchicine, also have similar modes of action. In this report we have correlated the cytotoxicity of combretastatins against the murine leukemic cell line L1210 with physicochemical parameters such as the summation of the Hansch-Fujita π constant, which was used as an index of lipophilicity of the substituent groups on ring A (Σπa) and ring B (Σπb), the vector summation of the group dipole moments of ring A (Σµa) and ring B (Σµb), the nature of the linker chain between ring A and ring B (Bt-L), indicator parameters (NOH)a and (NOH)b, which represent the number of hydroxyl groups on ring A and ring B, respectively, and the summation of π values of the substituents on the linker (ΣπL). Cytotoxicity correlated well with (Σπb), (NOH)a, (Bt-L), and (Σµb), and the dependency on (Σπb) was found to be parabolic.

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Authors and Affiliations

  1. Department of Pharmaceutical Sciences, School of Pharmacy, University of Southern California, 1985 Zonal Avenue, Los Angeles, California, 90033

    Partha Nandy, Samitendu Banerjee, Hua Gao, Mary B. V. Hui & Eric J. Lien

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  1. Partha Nandy
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  2. Samitendu Banerjee
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  3. Hua Gao
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  4. Mary B. V. Hui
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  5. Eric J. Lien
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Nandy, P., Banerjee, S., Gao, H. et al. Quantitative Structure–Activity Relationship Analysis of Combretastatins: A Class of Novel Antimitotic Agents. Pharm Res 8, 776–781 (1991). https://doi.org/10.1023/A:1015814403997

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