engleski

New heterocycles from benzothiazole series ; sythesis and antitumor activity

Novi heterocikli iz reda benzotiazola : sinteza i antitumorska aktivnost = new heterocycles from benzothiazole series : sythesis and antitumor activity / Grace Karminski-Zamola, Faculty of Chemical Engineering and Technology, Department of Organic Chemistry, Marulićev trg 20, HR-10000 Zagreb ; gzamola@fkit.hr Despite major breakthroughs in diagnosis and treatment, cancer is still the second leading cause of death in the Western world. The discovery and development of new, more active, more selective, and less toxic compounds for the treatment of malignancy are one of the most important goals in medicinal chemistry. Newly synthesized benzothiazoles demonstrate interesting pharmacological activities and led to development of new medications for treating diseases. They were studied extensively for their antiallergic, anti-inflammatory, , 10 antitumor11-14 and other biological activities.15, 16 The above considerations prompted us to design and synthesize a new series of amidino-substituted benzothiazole derivatives (Figure 1) and to test their antiproliferative activity of tumor cells in vitro. [1] Ban, M. ; Taguchi, H. ; Katsushima, T. ; Takahashi, M. ; Shinoda, K. ; Watanabe, A. ; Tominaga, T. Bioorg. Med. Chem. 1998, 6, 1069–1076. [2] Papadopoulou, C. ; Geronikaki, A. ; Hadjipavlou-Litina, D. Farmaco 2005, 60, 969–973. [3] Chung, Y. ; Shin, Y.-K. ; Zhan, C.-G. ; Lee, S. ; Cho, H. Arch.Pharmacal Res. 2004, 27, 893–900. [4] Ćaleta I. ; Kralj M. ; Marjanović M. ; Branimir Bertoša B. ; Tomić S. ; Pavlović G. ; Pavelić K. and Karminski-Zamola G. J. Med. Chem., 2009, 52, 1744-1756 [5].Racane L. ; Tralić-Kulenović V. ; Kraljević Pavelić S. ; Ratkaj I. ; Peixoto P. ; Nhili R. ; Depauw S. ; Hildebrand MP. ; David-Cordonnier MH. ; Pavelić K. and Karminski-Zamola G, J. Med. Chem. 2010, 53, 2418-2432

benzothiazoles; antitumor activity

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