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Synthesis and Anticancer Activity of Novel Urea and Thiourea Bearing Thiophene-2-carboxalate Derivatives

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Abstract

A new series of urea and thiourea bearing thiophene-2-carboxalate derivatives has been designed against protein tyrosine phosphatase 1B (PTP1B) active site, synthesized and charecterized by 1H and 13C NMR, and mass spectra. The compounds have been evaluated for in vitro anticancer activity against different cancer cell lines using the MTT colorimetric assay and doxorubicin as a standard drug. Among the tested compounds, methyl 3-methoxy-4-{4-[3-(4-methoxyphenyl)thioureido]phenyl}thiophene-2-carboxylate demonstrates the highest inhibitory activity against MCF-7, K562, HepG2, MDA-MB-231, and HeLa cell lines. The new molecular structures and their interactions with PNP1B have been evaluated by docking studies.

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ACKNOWLEDGMENTS

The authors would like to thank the management of AMRI Hyderabad research centre for giving an opportunity to carry out this research. The authors are also thankful to Sai Innotech Labs Pvt.Ltd.for providing synthesis facility.

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Authors and Affiliations

  1. Department of Chemistry, Koneru Lakshmaiah Education Foundation, Green Fields, Vaddeswaram, 522502, Guntur, India

    K. Ch. Gulipalli, S. Bodige, S. Endoori, P. Koteswara Rao Cherukumalli & N. Seelam

  2. Department of Pharmaceutical Chemistry, Gurunanak Institutions Technical Campus, School of Pharmacy, 501506, Hyderabad, India

    P. Ravula

  3. Department of Pharmaceutical Chemistry, Gurukrupa Institute of Pharmacy, 431129, Maharashtra, India

    J. N. Narendra Sharath Chandra

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  1. K. Ch. Gulipalli
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  2. P. Ravula
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Correspondence to N. Seelam.

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Gulipalli, K.C., Ravula, P., Bodige, S. et al. Synthesis and Anticancer Activity of Novel Urea and Thiourea Bearing Thiophene-2-carboxalate Derivatives. Russ J Gen Chem 90, 1336–1344 (2020). https://doi.org/10.1134/S1070363220070221

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