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Synthesis of indole based novel small molecules and their in vitro anti-proliferative effects on various cancer cell lines

( 2014-01-22) Dulla, Balakrishna ; Sailaja, E. ; Reddy Ch, Upendar ; Aeluri, Madhu ; Kalle, Arunasree M. ; Bhavani, S. ; Rambabu, D. ; Rao, M. V.Basaveswara ; Pal, Manojit

Indole based novel small molecules were designed as potential anticancer agents. Multi step synthesis of these compounds was carried out by using Pd/C-Cu mediated coupling-cyclization strategy as a key step. The single crystal X-ray diffraction study was used to confirm the molecular structure of a representative compound unambiguously. Many of these compounds were evaluated for their anti-proliferative properties in vitro against six cancer cell lines as well as noncancerous cells. All these compounds showed selective growth inhibition of cancer cells and several of them were found to be promising with IC50 values in the range of 0.1-1.2 μM, comparable to the known anticancer drug doxorubicin. © 2014 Elsevier Ltd. All rights reserved.