Cytotoxicity Evaluation of a New Set of 2-Aminobenzo[de]iso-quinoline-1,3-diones

Abstract

A new series of 2-amino-benzo[de]isoquinoline-1,3-diones was synthesized and fully characterized in our previous paper. Here, their cytotoxic effects have been evaluated in vitro in relation to colon HCT-116, hepatocellular Hep-G2 and breast MCF-7 cancer cell lines, using a crystal violet viability assay. The IC50-values of the target compounds are reported in µg/mL, using doxorubicin as a reference drug. The findings revealed that compounds 14, 15, 16, 21 and 22 had significant cytotoxic effects against HCT-116, MCF-7 and Hep-G2 cell lines. Their IC50 values ranged between 1.3 and 8.3 μg/mL in relation to doxorubicin (IC50 ≈ 0.45–0.89 μg/mL). Therefore, these compounds could be used as templates for furthering the development and design of more potent antitumor agents through structural modification.

Synthesis and biological evaluation of 4-(1H-1,2,4-triazol-1-yl)benzoic acid hybrids as anticancer agents

“…Synthetic routes for the formation of 1,2,4-triazole benzoic acid hybrids (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17) are shown in Scheme 1. Briey, 4-hydrazinobenzoic acid was reacted with dialkyl-N-cyanoimido(dithio)carbonate to derive 1,2,4-triazole benzoic acids 1 and 2 in good yields.…”

“…Therefore, strategic therapies for cancer continues to be a fascinating challenge and remain among the most urgent areas of research in medicinal chemistry. [1][2][3] The exploration of new heterocyclic compounds that exhibit potency for multiple biological purposes remains an intriguing scientic effort. For instance, triazoles and their annulated heterocycles have received great interest owing to their synthetic and pharmacophore features, and potential applicability to a range of bioactivities, such as anticancer, antibacterial, antiviral, and anti-inammation activities.…”

“…[4][5][6][7][8][9][10][11][12][13][14] Recently, we reported that triazoloquinazolines, which are derived from the combination of triazole and quinazoline, constitute an interesting antitumor class of compounds. For instance, 3-pyridyl-bis- [1,2,4]triazoloquinazoline and 5-ethoxytriazoloquinazoline have shown the highest cytotoxicity against Hep-G2 and colon HCT-116 carcinoma cells. 15 Furthermore, 5-chloro- [1,2,4] triazoloquinazolines have been found to possess promising anticancer activities against medulloblastoma (Daoy) and melanoma (SK-MEL28) cell lines.…”

“…For instance, 3-pyridyl-bis- [1,2,4]triazoloquinazoline and 5-ethoxytriazoloquinazoline have shown the highest cytotoxicity against Hep-G2 and colon HCT-116 carcinoma cells. 15 Furthermore, 5-chloro- [1,2,4] triazoloquinazolines have been found to possess promising anticancer activities against medulloblastoma (Daoy) and melanoma (SK-MEL28) cell lines. [16][17][18] Letrozole and anastrozole containing a 1,2,4-triazole ring have been approved by the FDA and used as rst-line therapies for the treatment of breast cancer in postmenopausal women owing to their apparent superiority to estrogen receptor antagonists, such as tamoxifen.…”

“…6 Based on the above information and our interest in determining the anticancer pharmacological activities of triazole compounds, we incorporated benzoic acid and the triazole pharmacophore into one molecule to generate novel 1,2,4-triazole benzoic acid hybrid scaffolds. Herein, we aim to describe the synthesis of seventeen hybrids (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17) and evaluate their in vitro antiproliferative activity against HCT-116 and MCF-7 human cancer cell lines, and normal human RPE-1 cells.…”