Antitumor evaluation and molecular docking study of substituted 2-benzylidenebutane-1,3-dione, 2-hydrazonobutane-1,3-dione and trifluoromethyl-1H-pyrazole analogues

Ibrahim A. Al-SuwaidanDepartment of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia,

Naglaa I. Abdel-AzizDepartment of Medicinal Chemistry, Faculty of Pharmacy, University of Mansoura, Mansoura, Egypt,

Adel S. El-AzabDepartment of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia, ;Department of Organic Chemistry, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt, and

Magda A.-A. El-SayedDepartment of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, University of Mansoura, Mansoura, Egypt

Amer M. AlanaziDepartment of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia,

Mahmoud B. El-AshmawyDepartment of Medicinal Chemistry, Faculty of Pharmacy, University of Mansoura, Mansoura, Egypt,

Alaa A.-M. Abdel-AzizDepartment of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia, ;Department of Medicinal Chemistry, Faculty of Pharmacy, University of Mansoura, Mansoura, Egypt, Correspondence[email protected]

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Antitumor evaluation and molecular docking study of substituted 2-benzylidenebutane-1,3-dione, 2-hydrazonobutane-1,3-dione and trifluoromethyl-1H-pyrazole analogues

Table 1. Antitumor activity of chalcone, hydrazone and pyrazole derivatives 2–7, 8, 10 and 13–16 presented as growth inhibition percentages (GI%) over 60 subpanel tumor cell lines.

Table 2. Antitumor activity of the most active chalcone, hydrazone and pyrazole 3, 5, 7, 8 and 16 with GI% over the most sensitive tumor cell line.

Table 3. Compounds 8 and 5-Flu median growth inhibitory (GI₅₀, µM), total growth inhibitory (TGI, µM) and median lethal (LC₅₀, µM) concentration of in-vitro subpanel tumor cell lines.

Table 4. GI₅₀ values (µM) of compound 8, gefitinib and erlotinib over the most sensitive cell lines of non-small lung cancer, colon cancer, melanoma, breast cancer, CNS cancer and leukemia subpanels.

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Antitumor evaluation and molecular docking study of substituted 2-benzylidenebutane-1,3-dione, 2-hydrazonobutane-1,3-dione and trifluoromethyl-1H-pyrazole analogues

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Table 1. Antitumor activity of chalcone, hydrazone and pyrazole derivatives 2–7, 8, 10 and 13–16 presented as growth inhibition percentages (GI%) over 60 subpanel tumor cell lines.

Table 2. Antitumor activity of the most active chalcone, hydrazone and pyrazole 3, 5, 7, 8 and 16 with GI% over the most sensitive tumor cell line.

Table 3. Compounds 8 and 5-Flu median growth inhibitory (GI50, µM), total growth inhibitory (TGI, µM) and median lethal (LC50, µM) concentration of in-vitro subpanel tumor cell lines.

Table 4. GI50 values (µM) of compound 8, gefitinib and erlotinib over the most sensitive cell lines of non-small lung cancer, colon cancer, melanoma, breast cancer, CNS cancer and leukemia subpanels.

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Table 3. Compounds 8 and 5-Flu median growth inhibitory (GI₅₀, µM), total growth inhibitory (TGI, µM) and median lethal (LC₅₀, µM) concentration of in-vitro subpanel tumor cell lines.

Table 4. GI₅₀ values (µM) of compound 8, gefitinib and erlotinib over the most sensitive cell lines of non-small lung cancer, colon cancer, melanoma, breast cancer, CNS cancer and leukemia subpanels.