Synthesis and anticancer and cytotoxic effects of novel 1,4-phenylene-bis-N-thiocarbamoylpyrazole and 1,4-phenylene-bis-pyrazolylthiazole derivatives

Abstract

Thiazolylpyrazoline derivatives were recently reported as potent anticancer agents. In this study, novel 1,4-phenylene-bis-N-thiocarbamoylpyrazoles (3a-h) and 1,4-phenylene-bis-pyrazolylthiazoles (5a-h) were prepared and screened for their anticancer activities against C6 (rat brain tumor cells) and HeLa (human uterus carcinoma). Anticancer activity studies were performed as a dose-dependent assay starting with eight concentrations. 5-Fluorouracil (5-FU) was used as a positive control. Compounds 3c, 3d, and 3h were examined and they revealed almost the same activities compared with 5-FU in terms of cell selectivity against C6 cells. Moreover, compounds 3a-h had lower cytotoxicity than 5-FU. The low cytotoxicity values of 3a-h as well as their high antiproliferative activity were encouraging, but further studies are required on the use of these molecules as anticancer drugs.

Development of PVC membrane potentiometric sensor for the determination of potassium ion and its applications

“…In this study, the synthesis of 5,5'-(1,4-phenylene)bis(3-(4methoxyphenyl)-4,5-dihydro-1H -pyrazole-1-carbothioamide) molecule was performed according to a previously published method [20] and spectroscopic data of the molecule is identical to that reported in the literature.…”

Determination of the inhibition profiles of pyrazolyl–thiazole derivatives against aldose reductase and α‐glycosidase and molecular docking studies

“…The reaction of 1a-i, which is performed according to the published procedure, [56,57] with 2,4′-dibromoacetophenone (2) in ethanol at reflux conditions for 1 hr gave the pyrazolyl-thiazole derivatives (3a-i) in high yields (70-92%; Scheme 1). [56,58] The structures of compounds 3a-i were explained on the basis of spectral data (IR and NMR) and elemental analysis. All spectral data were in good agreement with the proposed structures.…”

Synthesis, characterization, in vitro antiproliferative and cytotoxicity effects of a new class of 2-((1R,2S)-2-((E)-4-substitutedstyryl) cyclooctyl)benzo[d]thiazole derivatives

“…The 1 H NMR spectra of thiazoles (12)(13)(14), in each case, showed characteristic signals for thiazole ring at δ 8.00 The antiproliferative activities of the compounds 12-14 were determined against rat brain carcinoma (C6) and human cervical carcinoma (HeLa) cell lines using BrdU cell proliferation ELISA assay [32][33][34][35]. The antiproliferative activities of 12-14 and the controls were investigated on 5, 10, 20, 30, 40, 50, 75 and 100 µM concentrations and 5-Fluorouracil (5-FU) was chosen as a positive control due to its availability, and widespread using.…”

“…Antiproliferative activities of the compounds were investigated on HeLa and C6 cell lines using proliferation BrdU ELISA assay, [32][33][34][35] 5-FU was used as positive controls. The results are are presented as means ± SD of six values (p < 0.01).…”