Design, Synthesis and Antiproliferative Activities Evaluation of Thiazolopyrimidines Derivatives through Biginelli Reaction

Author(s): Pengju Zhu, Huansheng Fu, Hao Fang*

Journal Name: Letters in Drug Design & Discovery

Volume 14 , Issue 12 , 2017

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Graphical Abstract:


Background: Thiazolopyrimidines possessed their structural diversity and various biological activity. Up to date, thiazolopyrimidines derivatives have widespread applications in pharmaceutical fields. In this article, a series of thiazolopyrimidine derivatives were designed based on the lead compound structure in our previous studies.

Methods: All the target compounds were synthesized with the coupling reaction, Biginelli reaction and “one-pot” aldol condensation. Their structures were identified by 1H NMR, 13C NMR spectra and HRMS. Antitumor activities of the target compounds were evaluated by MTT.

Results: 25 new target compounds were synthesized and they primarily screened through testing their inhibitory rates against two human tumor cell lines and Compounds 15, 17, 20, 22, 40 exhibited more than 70% inhibitory rate against both MDA-MB-231 and K562. Further assessing their IC50 against five tumor cell lines, 15 and 22 show advantage over lead compound I in MDAMB- 231, K562 and PC-3.

Conclusion: A series of thiazolopyrimidine derivatives were synthesized and the preliminary biological evaluation suggest that target compound 22 exhibited better antiproliferative activity against K562 than gossypol.

Keywords: Thiazolopyrimidines, Biginelli reaction, antitumor, biological activity, K562, antiproliferative.

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Article Details

Year: 2017
Published on: 30 October, 2017
Page: [1382 - 1390]
Pages: 9
DOI: 10.2174/1570180814666170512123132
Price: $65

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