Literature DB >> 35852708

Rational synthesis, anticancer activity, and molecular docking studies of novel benzofuran liked thiazole hybrids.

Sanjay D Hadiyal1,2, Jaydeep N Lalpara2, Bhavin B Dhaduk2, H S Joshi3.   

Abstract

A novel series of benzofuran bearing thiazole hybrids were synthesized by the multistep reaction approach. All synthesized molecules were selected by the National Cancer Institute, USA for one-dose anticancer activity against 60 various human cancer cell lines indicating nine types of cancer. Among thirteen compounds, two compounds showed higher lethality, so, it was selected for five-dose anticancer screening against all cancer cell lines. Compound 8g and 8h were displayed remarkable antiproliferative activity with GI50 values ranging from 0.295 to 4.15 μM and LC50 values ranging from 4.43 to > 100 μM. All data are compared with standard drugs fluorouracil and doxorubicin. Compound 8g showed higher potency as a cytotoxic molecule then fluorouracil. Furthermore, all new hybrids were studied for molecular docking into the active binding sites of 1HOV protein.
© 2022. The Author(s), under exclusive licence to Springer Nature Switzerland AG.

Entities:  

Keywords:  Anticancer activity; Benzofuran; Molecular docking; NCI-60; Thiazole

Year:  2022        PMID: 35852708     DOI: 10.1007/s11030-022-10493-7

Source DB:  PubMed          Journal:  Mol Divers        ISSN: 1381-1991            Impact factor:   3.364


  1 in total

1.  Synthesis and antihypertensive activity of imidazo[2,1-b]-thiazoles bearing a 2,6-dichlorophenyl group.

Authors:  A Andreani; M Rambaldi; A Locatelli; A Cristoni; S Malandrino; G Pifferi
Journal:  Acta Pharm Nord       Date:  1992
  1 in total

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