Taurine-Based Hybrid Drugs as Potential Anticancer Therapeutic Agents: In Vitro, In Vivo Evaluations
Nakypova S. Smolobochkin A. Rizbayeva T. Turmanov R. Gazizov A. Akylbekov N. Zhapparbergenov R. Narmanova R. Ibadullayeva S. Zalaltdinova A. Syzdykbayev M. Voronina J. Lyubina A. Voloshina A. Klimanova E. Sashenkova T. Mishchenko D. Burilov A.
July 2025Multidisciplinary Digital Publishing Institute (MDPI)
Pharmaceuticals
2025#18Issue 7
Background/Objectives: The development of antitumor agents possessing low toxicity against non-cancerous cells is still a challenge in medicinal chemistry. In this paper, we report the antitumor activity of “hybrid structures” derived from the amino acid taurine. We have synthesized 26 compounds, structures of which were confirmed using NMR, X-ray diffractometry, and other techniques. Cytotoxicity of the obtained compounds has been evaluated using three human cancer cell lines. Pyrrolidine 4p has exhibited the strongest antiproliferative activity against HL-60 cells with an IC50 of 76.7 μM, while IC50 against normal cells was 176.3 μM. Water-soluble derivatives of taurine have been tested for antileukemia activity in mice of the BDF1 line. Compound 4p has been identified as the leading compound, which increases the mean survival time of mice from 40 to 100% as compared to the control group. Together, these results prove that taurine-based hybrid structures can be a promising scaffold for the discovery of potential antiproliferative agents.
anticancer agents , aza-Michael reaction , pyrrolidine , taurine
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Faculty of Chemistry and Chemical Technology, Al Farabi Kazakh National University, Al-Farabi Avenue 71, Almaty, 050040, Kazakhstan
Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Academician Arbuzov Street 8, Kazan, 420088, Russian Federation
Department of Chemistry, Abai Kazakh National Pedagogical University, Dostyk Avenue 13, Almaty, 050010, Kazakhstan
Laboratory of Engineering Profile “Physical and Chemical Methods of Analysis”, Korkyt Ata Kyzylorda University, Aiteke Bi Street 29A, Kyzylorda, 120014, Kazakhstan
“CNEC” LLP, Dariger Ali Lane 2, Kyzylorda, 120001, Kazakhstan
N.S. Kurnakov Institute of General and Inorganic Chemistry, Russian Academy of Sciences, Leninskii Avenue 31, Moscow, 119991, Russian Federation
Federal Research Center of Problems of Chemical Physics and Medicinal Chemistry, Russian Academy of Sciences, Academician Semenov Avenue 1, Chernogolovka, 142432, Russian Federation
Faculty of Fundamental Physical-Chemical Engineering, M.V. Lomonosov Moscow State University, Leninskiye Gory 1, Moscow, 119991, Russian Federation
Research and Educational Center in Chkrnogolovka, State University of Education, Radio Street 10a, Moscow, 105005, Russian Federation
Faculty of Chemistry and Chemical Technology
Arbuzov Institute of Organic and Physical Chemistry
Department of Chemistry
Laboratory of Engineering Profile “Physical and Chemical Methods of Analysis”
“CNEC” LLP
N.S. Kurnakov Institute of General and Inorganic Chemistry
Federal Research Center of Problems of Chemical Physics and Medicinal Chemistry
Faculty of Fundamental Physical-Chemical Engineering
Research and Educational Center in Chkrnogolovka
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