Synthesis and Cytotoxic Evaluation of 6‐(3‐Pyrazolylpropyl) Derivatives of 1,4‐Naphthohydroquinone‐1,4‐diacetate

Abstract

Several new 6-(3-pyrazolylpropyl) derivatives of 1,4-naphthohydroquinone-1,4-diacetate (NHQ-DA) have been prepared by chemical modifications of the Diels-Alder adduct of alpha-myrcene and 1,4-benzoquinone. All these new compounds and precursors have been evaluated in vitro for their cytotoxicity against cultured human cancer cells of MB-231 breast-adeno carcinoma, A-549 lung carcinoma, and HT-29 colon carcinoma. GI(50) values ranged in and below the micromolar concentration level.

Synthesis and Cytotoxicity of Bis‐1,3,4‐oxadiazoles and Bis‐pyrazoles Derived from 1,4‐Bis[5‐thio‐4‐substituted‐1,2,4‐triazol‐3‐Yl]‐butane and Their DNA Binding Studies

“…The standard MTT assay was used to determine IC 50 values i.e. the drug concentration that causes 50% cell-growth inhibition after 72 h of continued exposure to the test compounds and the mean of the results obtained from triplicate assays are shown in Table 2 [ [22][23][24]. The IC 50 data reported in Table 2 indicate that the bistriazoles substituted with 1,3,4-oxadiazole moiety 7-12 did not show significant anticancer activity where as the bis-triazoles substituted with pyrazole moiety 14, 15, and 16 exhibited higher cytotoxic activity against all the tested cell lines as indicated by lower IC 50 values.…”

“…The cell lines were procured from National Centre for Cell Sciences, Pune, India, and were cultured in DMEM medium supplemented with 10% FBS, 1% L-glutamine and 50 mg/mL gentamicin sulphate in a CO 2 incubator in a humidified atmosphere of 5% CO 2 and 95% air. The in-vitro cytotoxicity was determined using a standard MTT assay [22][23][24]. Briefly, the exponentially growing cells were plated in 96-well plates (10 4 cells/well in 100 mL of medium) and incubated for 24 h for attachment.…”

Synthesis, in vitro cytotoxicity, and anti-microbial studies of 1,4-bis(4-substituted-5-mercapto-1,2,4-triazol-3-yl)butanes

“…The standard MTT assay was used to determine IC 50 values, i.e., the drug concentration that causes 50% cell growth inhibition after 72 h of continuing exposure to the test compounds and the mean of the results obtained from triplicate assays are shown in Table 2 (Molinari et al, 2009;Manjula et al, 2009). The IC 50 values were compared with that of anti-cancer antibiotic doxorubicin.…”

“…The in vitro cytotoxicity was determined using a standard MTT assay (Molinari et al, 2009, Manjula et al, 2009. Briefly, the exponentially growing cells were plated in 96-well plates (10 4 cells/well in 100 ll of medium) and incubated for 24 h for attachment.…”

Novel 1<i>H</i>-Pyrazole-3-carboxamide Derivatives: Synthesis, Anticancer Evaluation and Identification of Their DNA-Binding Interaction

“…[13][14][15][16][17] All these greatly promote the progress of research in pyrazole compounds and recently such scaffold is not only employed in developing various kinase inhibitors, 10) but also in molecules that directly interact with DNA stands, such as metal complexes, alkylating agents, dimeric analogues, polyamide derivatives and some pyrazolefused derivatives. [18][19][20][21][22][23][24][25] The unexpected interaction between DNA and pyrazole-derived kinase inhibitors can cause offtarget effects, including potential improvement of cell toxicity and anticancer activity. Pyrazole ring can form a rigid plane with electron-rich system chromophores and embed into the DNA minor grooves to make a π-π stacking with DNA bases, [26][27][28] which is usually essential for the DNA-binding.…”