Synthesis, characterization and anticancer evaluation of some new triazole derivatives

Sunil, Dhanya (2012) Synthesis, characterization and anticancer evaluation of some new triazole derivatives. Phd. Thesis thesis, Manipal Institute of Technology, Manipal.

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Cancer characterized by uncontrolled, rapid and pathological proliferation of abnormal cells, is the second leading cause of death in humans after cardiovascular diseases in developing as well as advanced countries. Although there are many therapeutic strategies including chemotherapy and radiotherapy, high toxicity and drug resistance limit the positive outcomes in most cases. Moreover most of the chemotherapeutic drugs are expensive. Therefore, novel diagnosis, treatment and prevention approaches are urgently needed for cancer therapy. Research in this direction is still going on, to find an alternative drug which can target the malignant tissues, less toxic and affordable by common man. 1,2,4-triazole derivatives exhibit a wide spectrum of biological activities such as antibacterial, antifungal, antiviral, anticancer etc. The aromatic inhibitors like Anastrazole and Letrozole, which are currently used in the treatment of metastatic breast cancer, are triazole derivatives. Triazole is an important emerging moiety in pharmaceutical study and a lot of work can be carried out on this molecule for obtaining better therapeutic activity. Drugs based on a pyrazole ring have often been occupying a position in the list of best-selling pharmaceutical products since last few decades. Many pyrazole derivatives have been reported to display an array of diverse pharmacological activities such as anti-inflammatory, antimicrobial, antihypertensive, tuberculostatic, analgesic, antidiabetic, antileishmanial and antitumor. Prompted by the therapeutic importance of 1,2,4-triazoles and pyrazoles, it was intended to synthesize five series of triazole derivatives: Schiff bases, Mannich bases, Thiadiazoles, Thiazolidinones and Thiadiazepines which incorporated the bioactive pyrazole moiety. The structures of the newly synthesized molecules were confirmed by IR, 1H-NMR, mass spectra and C,H,N analyses. The in vitro antioxidant and anticancer studies of the triazole derivatives were carried out. The mechanism of anticancer and antioxidant activity of the most potent molecules were studied. The in vivo anticancer and toxicity studies of the molecules that were active in vitro were also assessed.

Item Type: Thesis (Phd. Thesis)
Uncontrolled Keywords: Triazole, Pyrazole, Schiff bases, Mannich bases, Thiadiazoles, Thiazolidinones, Thiadiazepines, Anticancer studies, Antioxidant studies
Subjects: Engineering > MIT Manipal > Chemistry
Depositing User: MIT Library
Date Deposited: 23 Mar 2016 08:55
Last Modified: 23 Mar 2016 08:55

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