Synthesis and characterization of new 1,2,4-triazole anticancer scaffold derivatives: In Vitro study

Abstract

Four Schiff bases were obtained via one direct click reaction between 3-amino-1H-1,2,4-triazole and different substituted benzaldehyde. The synthesized compounds were characterized on the basis of their spectral data including IR spectra, mass spectroscopy and 1 HNMR. The synthesized compounds were tested against three human cancer cell lines to evaluate their in vitro anticancer activity, and also tested on Vero cells extracted from African green monkey kidney to investigate their side effect. The screening showed that the Schiff bases TB-NO2 and TB-OCH3 produced an effective anticancer activity against HEPG2, HCT-116, and MCF-7 cell lines. Further investigations had been conducted to determine the apoptotic and antifibrotic ability of TB-NO2 and TB-OCH3 on MCF-7 cells by determining the expression of Bax, Bcl-2, CTGF, and PDGF. Results of Bax/Bcl-2 ratio for TB-NO2 and TB-OCH3 confirmed the apoptotic effect of these compounds on MCF-7 cells. The reduction in CTGF and PDGF genes expression confirmed the regulatory effect of these compounds on MCF-7 cells growth.

Synthesis of Manganese(II), Iron(III), and Vanadium(IV) Complexes with New Schiff Bases and their Spectroscopic and Thermal Studies and Evaluation of their Antimicrobial Activity

“…According to previous studies, which revealed that coumarin, chalcone fibrates can down-regulate the total cholesterol (TC), phospholipids (PL) and triglycerides (TG) and regulate the levels of VLDL, LDL, and HDL, on the other side, pyrimidine serves an essential function in human proliferation as ribonucleotide bases in RNA and as deoxyribonucleotide bases in DNA, and it has been found to contribute to multiply biological activates (7). They are considered powerful tools for treatments and possess broad, interesting biological activities such as anti-tumor and anti-fungal and they are used for thyoid drugs and leukemia (8).…”