Design and Synthesis of Novel Thiazole Linked Tetrahydropyridine Analogues as Anticancer Agents

A library of new thiazole linked tetrahydropyridines (6a-q) synthesized and screened for their invitro anticancer activity against human breast adeno carcinoma cell viz. MCF-7 and MDA-MB-231. The two compounds 6d containing -F and -Cl functions in para and meta position of phenyl ring (9.94 +/- 1.02 mu M, 9.78 +/- 1.08 mu M) and 6e with -Cl and -NH2 functions on pyridine ring (9.72 +/- 0.91 mu M, 9.54 +/- 0.95 mu M) demonstrated outstanding activity against both the cell lines when compared to Doxorubicin. The benzofuran analogue 6o presented good activity with an IC50 value of 12.19 +/- 1.03 mu M (MCF-7) and 12.22 +/- 1.07 mu M (MDA-MB-231). The molecular docking study of potent molecule 6e against crystal structure of breast tumor kinase presented promising docking score and binding interactions. Predicted pharmacokinetics properties of compounds 6a-q and presented boiled diagram of compounds 6d and 6e implied favourable drug-likeness properties.