Synthesis and antiproliferative activities of some pyrazole-sulfonamide derivatives

Abstract

In this study, a series of pyrazole-sulfonamide derivatives were designed and synthesized from 1-(4-aminophenyl)-4-benzoyl-5-phenyl-N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)-1H-pyrazole-3-carboxamide (1). The newly synthesized sulfonamides were characterized by FT-IR, 1 H NMR, 13 C NMR, and elemental analyses. The compounds were tested for their in vitro antiproliferative activities against HeLa and C6 cell lines. The tests were carried out as dose-dependent assay starting from 5 to 100 lg/mL. All compounds showed especially cell selective effect against rat brain tumor cells (C6). Some of the tested compounds (3) and (7) showed promising broad spectrum antitumor activity comparable to the activities of the commonly used anticancer drugs, 5-fluorouracil and cisplatin.

Antiproliferative Activity of New Pyrazole-4-sulfonamide Derivatives: Synthesis and Biological Evaluation

“…There has always been a need to get novel series of compounds, which exhibits good antiproliferative or cytotoxic compounds that displayed distinct antiproliferative properties. − Exploring small molecule antitumor compounds, which could decrease drug resistance and reduce unnecessary side effects, is more desirable. These compounds are further tested to know any unwanted cytotoxic activity on these cancer cells, and the results showed that they were not cytotoxic, which might be safe.…”

“…Previously, a series of new pyrazole sulfonamide derivatives were reported elsewhere for their anticancer activity (Samet et al, 17 ). Most of the tested derivatives showed moderate to excellent activity against the tested-on rat brain tumor cell lines (C6).…”

Organoruthenium (II) complexes featuring pyrazole‐linked thiosemicarbazone ligands: Synthesis, DNA/BSA interactions, molecular docking, and cytotoxicity studies

“…Pyrazole‐pyrimidine derivatives have shown antiproliferative activity against NCl‐H226 (human lung carcinoma), NPC‐TW01 (nasopharyngeal cancer), T‐cell leukemia (Jurkat) cells, and a group of other human cancer cell lines. [ 1–3 ] A series of pyrazole–sulfonamide conjugates with antiproliferative activity against HeLa and C6 cell lines was reported by Mert et al [ 4 ] Via et al reported antiproliferative activities of benzothiopyranopyrazole derivatives exerted on HeLa and HL‐60 cells. [ 5 ] A phenyl, p ‐chlorophenyl, or p ‐methoxyphenyl substituent at 1‐position and a methoxy substituent at the 7‐position of the heterocyclic moiety was found to be responsible for the activities.…”

Regioselective lithiation of 1‐benzylpyrazole derivatives: Synthesis of amides derived from pyrazole

“…Over the past few decades much attention has been paid to nitrogen‐containing heterocycles. Amongst them, pyrazole derivatives have found numerous applications in many areas of chemistry . Various properties of pyrazole derivatives determine their usefulness.…”