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Research Article

A quantitative structure-activity relationship study of novel, potent, orally active, selective VEGFR-2 and PDGFRα tyrosine kinase inhibitors: Derivatives of N-Phenyl-N′-{4-(4-quinolyloxy)phenyl}urea as antitumor agents

B. K. Sharma Department of Chemistry, S K Government College, Sikar, 332 001

S. K. Sharma Department of Chemistry, S K Government College, Sikar, 332 001

P. Singh Department of Chemistry, S K Government College, Sikar, 332 001

Susheela Sharma Department of Engineering Chemistry, Sobhasaria Engineering College, Sikar, 332 021, INDIA

Figures & data

Figure 1 The derivatives of N-Phenyl-N′-{4-(4-quinolyloxy)phenyl}urea.

Table I. QSAR parameters and inhibitory activities of N-Phenyl-N′-{4-(4-quinolyloxy) phenyl}urea derivatives for VEGFR-2 and PDGFRα (see for structures).

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Table II. Stepwise development of Equation (1); pIC₅₀ = a₀ + a₁ClogP + a₂Es₂ + a₃F₃ + a₄HA₄ + a₅Es₆

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Table III. Intercorrelation Matrix^a among the predictors of Equation (1)

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Figure 2 Plot showing variation of observed versus calculated and predicted pIC₅₀ values.

Figure 2 Plot showing variation of observed versus calculated and predicted pIC50 values.

Table IV. Stepwise development of Equation (2); pIC₅₀ = b₀ + b₁ClogP + b₂R₃ + b₃I_X

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Table V. Intercorrelation Matrix^a among the predictors of Equation (3)

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A quantitative structure-activity relationship study of novel, potent, orally active, selective VEGFR-2 and PDGFRα tyrosine kinase inhibitors: Derivatives of N-Phenyl-N′-{4-(4-quinolyloxy)phenyl}urea as antitumor agents

Table I. QSAR parameters and inhibitory activities of N-Phenyl-N′-{4-(4-quinolyloxy) phenyl}urea derivatives for VEGFR-2 and PDGFRα (see for structures).

Table II. Stepwise development of Equation (1); pIC₅₀ = a₀ + a₁ClogP + a₂Es₂ + a₃F₃ + a₄HA₄ + a₅Es₆

Table III. Intercorrelation Matrix^a among the predictors of Equation (1)

Table IV. Stepwise development of Equation (2); pIC₅₀ = b₀ + b₁ClogP + b₂R₃ + b₃I_X

Table V. Intercorrelation Matrix^a among the predictors of Equation (3)

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A quantitative structure-activity relationship study of novel, potent, orally active, selective VEGFR-2 and PDGFRα tyrosine kinase inhibitors: Derivatives of N-Phenyl-N′-{4-(4-quinolyloxy)phenyl}urea as antitumor agents

Figures & data

Table I. QSAR parameters and inhibitory activities of N-Phenyl-N′-{4-(4-quinolyloxy) phenyl}urea derivatives for VEGFR-2 and PDGFRα (see Figure 1 for structures).

Table II. Stepwise development of Equation (1); pIC50 = a0 + a1ClogP + a2Es2 + a3F3 + a4HA4 + a5Es6

Table III. Intercorrelation Matrixa among the predictors of Equation (1)

Table IV. Stepwise development of Equation (2); pIC50 = b0 + b1ClogP + b2R3 + b3IX

Table V. Intercorrelation Matrixa among the predictors of Equation (3)

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Table I. QSAR parameters and inhibitory activities of N-Phenyl-N′-{4-(4-quinolyloxy) phenyl}urea derivatives for VEGFR-2 and PDGFRα (see for structures).

Table II. Stepwise development of Equation (1); pIC₅₀ = a₀ + a₁ClogP + a₂Es₂ + a₃F₃ + a₄HA₄ + a₅Es₆

Table III. Intercorrelation Matrix^a among the predictors of Equation (1)

Table IV. Stepwise development of Equation (2); pIC₅₀ = b₀ + b₁ClogP + b₂R₃ + b₃I_X

Table V. Intercorrelation Matrix^a among the predictors of Equation (3)