Recent development of imidazole derivatives as potential anticancer agents

Cancer, one of the key health problems globally, is a group of related diseases that share a number of characteristics primarily the uncontrolled growth and invasive to surrounding tissues. Chemotherapy is one of the ways for the treatment of cancer which uses one or more anticancer agents as per chemotherapy regimen. Limitations of most anticancer drugs due to a variety of reasons such as serious side effects, drug resistance, lack of sensitivity and efficacy etc. generate the necessity towards the designing of novel anticancer lead molecules. In this regard, the synthesis of biologically active heterocyclic molecules is an appealing research area. Among heterocyclic compounds, nitrogen containing heterocyclic molecules has fascinated tremendous consideration due to broad range of pharmaceutical activity. Imidazoles, extensively present in natural products as well as synthetic molecules, have two nitrogen atoms, and are five membered heterocyclic rings. Because of their countless physiological and pharmacological characteristics, medicinal chemists are enthused to design and synthesize new imidazole derivatives with improved pharmacodynamic and pharmacokinetic properties. The aim of this present chapter is to discuss the synthesis, chemistry, pharmacological activity, and scope of imidazole-based molecules in anticancer drug development. Finally, we have discussed the current challenges and future perspectives of imidazole-based derivatives in anticancer drug development.

Study on tri-imidazole derivatives modified with triazine-trione structure as latent curing agents for epoxy resin

In this paper, four novel kinds of triazine-trione based tri-imidazole derivatives (IM-TT, 2MI-TT, 2EI-TT and EMI-TT) were synthesized through the addition reaction between triglycidyl isocyanurate (TGIC) and imidazole (IM), 2-methylimidazole (2MI), 2-ethylimidazole (2EI) and 2-ethyl-4-methylimidazole (EMI), respectively. The triazine-trione based tri-imidazole derivatives were blended with epoxy resin and the reactivity, thermal latency and thermal property were investigated. The results on curing behaviors indicated that the curing exothermic peaks of the blends with triazine-trione based tri-imidazole derivatives shifted to higher temperatures compared with those with commercial imidazoles. The curing exothermic peak temperatures (Tps) of the synthesized tri-imidazole derivatives were increased by 23–32 ℃ compared with the unmodified imidazoles. In addition, Rheological behavior results indicated that the EP blends with tri-imidazole derivatives also exhibited excellent storage stability which was as long as 38 days under room temperature. Last but not the least, the EP blends with triazine-trione based tri-imidazole derivatives also exhibited high glass transition temperatures due to introducing of triazine-trione structures with high crosslinking density. The glass transition temperatures (Tgs) of the prepared thermosets ranged from 128 to 152 ℃. The triazine-trione based tri-imidazole derivatives provide a way to prepare latency epoxy resin with high high glass transition temperature and long storage stability. Article Highlights Four novel kinds of triazine-trione based tri-imidazole derivatives were synthesized. The EP cured with the tri-imidazole derivatives displayed great thermostability. The EP cured with the tri-imidazole derivatives exhibited long storage stability.

Hybrid Sol-Gel Matrices Doped with Colorimetric/Fluorimetric Imidazole Derivatives

Organic-inorganic hybrids (OIH) are materials that can be easily synthesized by the sol-gel method and combine the advantages of organic and inorganic moieties within a single polymeric matrix. Imidazole derivatives are versatile organic compounds that can change their optical properties with the variation of pH due to the protonation or deprotonation of the nitrogen atoms. This work reports the preparation of different OIHs doped with different contents of two imidazole compounds (3a,b). The obtained materials were characterized structurally by FTIR, and the dielectric properties were studied by electrochemical impedance spectroscopy. The optical properties were studied by UV-Vis absorption and fluorescence spectroscopies. The FTIR analysis showed that the presence of the imidazole does not change the structural properties of the matrices. The normalized resistance values obtained for the doped matrices ranged between 8.57 and 9.32 Ω cm2, all being higher than the undoped matrix. The σ ranged between 9.49 and 10.28 S cm−1, being all higher than the pure OIH samples. Compound 3a showed a maximum absorption peak at 390 nm, which is present in the OIH spectra, proving the presence of the compound. In the case of compound 3b, a maximum absorption wavelength at 412 nm was found, and the compound peak was not clear, which may indicate that an interaction between the compound and the matrix occurred. A synergetic effect between the intrinsic emission of the matrix and the fluorescence of 3a is found on the OIH-doped matrices.