The N-(2,4-diarylthiazol-5-yl)benzamidines library creation and the effect of this compounds on cancer cell growth-Reference-Cited by-同舟云学术

The N-(2,4-diarylthiazol-5-yl)benzamidines library creation and the effect of this compounds on cancer cell growth

Published:2022-12-30 Issue:2 Volume:17 Page:14-22
ISSN:1814-9766
Container-title:Ukrainica Bioorganica Acta
language:en
Short-container-title:Ukr. Bioorg. Acta

Author:

Severin Oleksandr O.¹^ORCID,Kachaeva Maryna V.¹^ORCID,Pilyo Stepan G.¹^ORCID,Shablykina Olga V.²^ORCID,Moskvina Viktoriia S.²^ORCID,Brovarets Volodymyr S.¹^ORCID

Affiliation:

1. V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the NAS of Ukraine, Kyiv, Ukraine

2. V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the NAS of Ukraine, Kyiv, Ukraine; Taras Shevchenko National University of Kyiv, Kyiv, Ukraine

Abstract

A versatile and efficient protocol for the synthesis of library of N-(2,4-diarylthiazol-5-yl)benzamidines is described. We obtained a library of 25 diversity with different of substituents in four positions in key framework. The synthesized amidine derivatives were evaluated for their in vitro anticancer activity. Analysis of anticancer activity on 60 cancer cell lines showed a decrease of proliferation of Colon Cancer and Leukemia cell lines by more than half and allowed to establish the structure-activity relationship

Funder

National Cancer Institute

National Institutes of Health

Enamine

Publisher

National Academy of Sciences of Ukraine (Co. LTD Ukrinformnauka) (Publications)

Reference21 articles.

1. Zhang T.Y. The Evolving Landscape of Heterocycles in Drugs and Drug Candidates. Advances in Heterocyclic Chemistry. 2017, 121, 1-12. https://doi.org/10.1016/bs.aihch.2016.05.001

2. Narasimhamurthy, K.H.; Sajith, A.M.; Joy, M.N.; Rangappa, K.S. An Overview of Recent Developments in the Synthesis of Substituted Thiazoles. Chemistry Select. 2020, 5, 5629-5656. https://doi.org/10.1002/slct.202001133

3. Zhang, Z.; Shu, B.; Zhang, Y.; Deora, G.S.; Li, Q.S. 2,4,5-Trisubstituted Thiazole: A Privileged Scaffold in Drug Design and Activity Improvement. Curr Top Med Chem. 2020, 20, 2535-2577. https://doi.org/10.2174/1568026620999200917153856

4. Borcea, A.M.; Ionuț, I.; Crișan, O.; Oniga, O. An Overview of the Synthesis and Antimicrobial, Antiprotozoal, and Antitumor Activity of Thiazole and Bisthiazole Derivatives. Molecules. 2021, 26, 624. https://doi.org/10.3390/molecules26030624

5. Scott, D.A.; Aquila, B.M.; Bebernitz, G.A.; Cook, D.J.; Dakin, L.A.; Deegan, T.L.; Maureen, M.H.; Stephanos, I.; Paul, D.L.; Charles, A.O.; Minwei, Y.; Zheng, X. Pyridyl and thiazolyl bisamide CSF-1R inhibitors for the treatment of cancer. Bioorg. Med. Chem. Lett. 2008, 18, 4794-4797. https://doi.org/10.1016/j.bmcl.2008.07.093