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A series of thiophene derivatives substituted at 2, 3 and 5 positions were designed and synthesized using 2,3-disubstituted thiophene aldehyde and alcohol as key building blocks. Invitro cytotoxicity assessed against PC-3, DU145 (prostate), A549 (lung), HT29, HCT116 (colon), MCF7, MDAMB231 (breast), B16F10 (melanoma) NCI (Colorectal) cancer cell lines by conducting (MTT) assay of thiophene derivatives. Most of these synthesized compounds showed anti-cancer activity, compound  5b  showed good cytotoxicity with IC 50  = 2.61 ± 0.34  µ M on HT29 cell line. Also, the key property of cell migration was observed while treating cells with  5b . The Cell cycle arrest at G2/M phase was observed by  5b  on HT29 cell line which inhibited tubulin polymerization with IC 50  value of 8.21 ± 0.30 μM. Moreover, binding pose with co-crystal ligand and interaction with colchicine binding site of  5b  was established by molecular docking studies. Hence this scaffold can be developed as anti-cancer agents that target tubulin polymerization.

Design, synthesis and molecular docking study of thiophenyl hydrazone derivatives as tubulin polymerization inhibitors