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Transient receptor potential canonical channel 6 (TRPC6) has been implicated in many kinds of malignant tumors, but very few potent TRPC6 antagonists are available. In this study, a benzothiazole amide derivative 1a was discovered as a TRPC6 activator in a cell-based high-throughput screening. A series of benzothiazole amide derivatives were designed and synthesized. The docking analyses indicated that the conformations of the compounds bound to TRPC6 determined the agonistic or antagonistic activity of the compounds against TRPC6, and compound 1s with the tetrahydronaphthalene group in R 1 position fit well into the binding pocket of the antagonist-bound conformation of TRPC6. Compound 1s showed an inhibitory potency order of TRPC3 (IC 50 3.3 ± 0.13 μM) ≈ C6 (IC 50 4.2 ± 0.1 μM) &gt; C7 with good anti-gastric cancer activity in a micromolecular range against AGS and MKN-45, respectively. In addition, 1s inhibited the invasion and migration of MKN-45 cells in vitro .

Benzothiazole Amides as TRPC3/6 Inhibitors for Gastric Cancer Treatment