The class of tubuline inhibitors is still not very well understood. This category shows potential in several classes of\ndrugs. We have exploited the nucleus for potential tubuline inhibitors. Chemical compounds that target microtubules and inhibit\nthe normal function of the mitotic spindle, have proven to be one of the best classes of cancer chemotherapeutic drugs available\nto date. Recently, combretastatin derivatives have therefore gained intense interest as potential antiproliferative agents. We\nhave used the scaffold of azetidinones to prepare structural analogues of combretastatin. A series of 1, 4 disubstituted 3 chloro 2\nazetidinones was designed using Surflex Dock (Tripos Inc.) software on the crystal structure of Tubuline (PDB entry-1SA0).\nGreen chemical synthesis of the designed series of 2-azetidinone analogues of combretastatin was undertaken using different\nsubstituted aromatic anilines and aldehydes as starting materials. The finished products have been characterized by melting\npoint, solubility and TLC and spectral analysis. The compounds have been tested for preliminary antiproliferative activity by a\nrapid, easy to perform assay method on Vigna radiata beans. The compounds have exhibited potential as anticancer activity.
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