Abstract

The synthesis of some new morpholine-benzimidazole-pyrazole hybrids (8a-o) and their in vitro anticancer activity against three human cancer cell lines like breast (MCF7), prostate (PC3) and lung (A549) was reported herein. Among all the hybrids, compound 8k displayed superior activity against all the cell lines than the standard drug etoposide. As well, compounds 8d, 8e, 8f and 8m showed most promising activity as compared to the positive control. Furthermore, compounds 8e, 8f, 8k were found to be 2 to 3 times more potent in inhibiting tubulin polymerization as compared to standard combretastatin A-4 (CA-4). Finally two in silico studies like molecular docking on α,β-tubulin (PDB ID-1SA0) and ADMET for the active compounds 8d, 8e, 8f, 8k and 8m were carried out, where, the results were found to be covenant with the corresponding anticancer data.

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