1003584-71-1Relevant academic research and scientific papers
Design, synthesis, and in vitro evaluation of cytotoxic activity of new substituted 1,4-benzoquinones and hydroquinones
Chaaban, Ibrahim,El-Khawass, El-Sayeda,Mahran, Mona,El-Sayed, Ola,El-Saidi, Hassan,Aboul-Enen, Hassan
, p. 49 - 77 (2008/12/21)
A new series of p-benzoquinones, hydroquinones, and quinol dimethyl ethers substituted by a pyrazole ring either directly or after an oxoethyl linker was synthesized and screened for in vitro cytotoxic activity. Compounds 8d, f, g, i, and 9c, f, and 13c exhibited broad-spectrum activity (GI50 MG-MID values 9.27-14.72 μM). With regard to sensitivity, compounds 8f and 9c, f have proved to possess a remarkable activity against leukemia tumor cell lines (GI50 = 3.43-5.03 μM). Indeed, compound 13c showed the highest activity profile against individual leukemia subpanel cell line SR (GI 50 = 0.91 μM).
1,3,5 trisubstituted pyrazole compounds for treatment of inflammation
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, (2008/06/13)
A class of 1,3,5-triaryl or heteroaryl pyrazoles is described for the treatment of inflammation, including treatment of pain and disorders such as arthritis. Compounds of particular interest are of Formula I STR1 wherein R1 is lower alkylsulfonyl or sulfamyl; wherein R2 is aryl or heteroaryl; wherein R2 is optionally substituted at substitutable positions with one or more radicals selected from halo, lower alkoxy, lower alkyl, nitro, lower alkylthio, amino, lower haloalkyl, hydroxyl, carboxyl, N-monoalkylamino, N,N-dialkylamino, cyano, alkoxycarbonyl and acylamino; wherein R3 is selected from hydrido, lower alkyl, lower haloalkyl, cyano, carboxyl, alkoxycarbonyl, amino, acyl, acylamino, halo and alkylsulfonylamino; wherein R4 is aryl or heteroaryl; wherein R4 is optionally substituted at a substitutable position with one or more radicals selected from halo, lower alkoxy, lower alkyl, nitro, lower alkylthio, amino, lower haloalkyl, hydroxyl, carboxyl, N-monoalkylamino, N,N-dialkylamino, cyano, alkoxycarbonyl and acylamino; provided R2 and R4 cannot be phenyl or substituted triazole, when R1 is sulfamyl; further provided R2 cannot be 4-methoxyphenyl or 4-methylphenyl when R4 is 4-methoxyphenyl or 4-methylphenyl and when R1 is sulfamyl; and further provided that R2 cannot be tetrazole when R4 is fluorophenyl, and when R1 is methylsulfonyl; or a pharmaceutically-acceptable salt thereof.
