Manar M Arafeh1, Ebrahim Saeedian Moghadam2, Sirin A I Adham3, Raphael Stoll4, Raid J Abdel-Jalil2. 1. Faculty of Pharmacy, Middle East University, Amman 11831, Jordan. 2. Chemistry Department, College of Science, Sultan Qaboos University, Muscat 123, Oman. 3. Biology Department, College of Science, Sultan Qaboos University, Muscat 123, Oman. 4. Biomolecular NMR, Ruhr University of Bochum, D-44780 Bochum, Germany.
Abstract
A novel series of 2-(aryldiazenyl)-3-methyl-1H-benzo[g]indole derivatives (3a-f) were prepared through the cyclization of the corresponding arylamidrazones, employing polyphosphoric acid (PPA) as a cyclizing agent. All of the compounds (3a-f) were characterized using 1H NMR, 13C NMR, MS, elemental analysis, and melting point techniques. The synthesized compounds were evaluated for cytotoxic activity against diverse human cancer cell lines by the National Cancer Institute. While all of the screened compounds were found to be cytotoxic at a 10 µM concentration, two of them (2c) and (3c) were subjected to five dose screens and showed a significant cytotoxicity and selectivity.
A novel series of n class="Chemical">2-(aryldiazenyl)-3-methyl-1H-benzo[g]indole derivatives (3a-f) were prepared through the cyclization of the corresponding arylamidrazones, employing polyphosphoric acid (PPA) as a cyclizing agent. All of the compounds (3a-f) were characterized using 1HNMR, 13CNMR, MS, elemental analysis, and melting point techniques. The synthesized compounds were evaluated for cytotoxic activity against diverse humancancer celllines by the NationalCancer Institute. While all of the screened compounds were found to be cytotoxic at a 10 µM concentration, two of them (2c) and (3c) were subjected to five dose screens and showed a significant cytotoxicity and selectivity.