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A multicomponent synthesis was empolyed for the synthesis of ethyl 2-amino-4,5,6,7-tetrahydrobenzo[ b ]thiophene-3-carboxylate 1 . An interesting cyclization was obtained when the amino-ester 1 reacted with ethyl isothiocyanate to give the benzo[4,5]thieno[2,3- d ][1,3]thiazin-4-one 3 . Acylation of the amino-ester 1 with chloroacetyl chloride in DCM and Et 3 N afforded the acylated ester 4 . The amino-ester 1 was cyclized to benzo[4,5]thieno[2,3- d ]pyrimidin-4(3 H )-one 8, which was reacted with some alkylating agents leading to alkylation at nitrogen 9-13 . Hydrazide 14 was utilized as a synthon for the synthesis of the derivatives 15 - 19 . Chloro-thieno[2,3- d ]pyrimidine 20 was synthesized and reacted with the hydrazine hydrate to afford the hydrazino derivative 21, which was used as a scaffold for getting the derivatives 22 - 28 . Nucleophilic substitution reactions were used for getting the compounds 29 - 35 from chloro-thieno[2,3- d ]pyrimidine 20 . In the way of anticancer therapeutics development, the requisite compounds were assessed for their cytotoxicity in vitro against MCF-7 and HepG-2 cancer cell lines. Twelve compounds showed an interesting antiproliferative potential with IC 50 from 23.2 to 95.9 µM. The flow cytometric analysis results showed that hit 4 induces the apoptosis in MCF-7 cells with a significant 26.86% reduction in cell viability. The in vivo study revealed a significant decrease in the solid tumor mass (26.6%) upon treatment with compound 4 . Moreover, in silico study as an agonist for inhibitors of JAK2 and prediction study determined their binding energies and predicted their physicochemical properties and drug-likeness scores.

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Discovery of New Apoptosis-Inducing Agents for Breast Cancer Based on Ethyl 2-Amino-4,5,6,7-Tetra Hydrobenzo[b]Thiophene-3-Carboxylate: Synthesis, In Vitro, and In Vivo Activity Evaluation