Project's information
| Project's title | Synthesis and investigation of properties of new condensed indolysines and indenes containing pharmacophore groups |
| Project’s code | QTRU01.05/21-22 |
| Research hosting institution | Institute of Chemistry |
| Coordinating unit, co-chair | Russian Foundation of Bacis Rearch |
| Project leader’s name | Assoc.Prof. Dr. Dang Thị Tuyet Anh and Prof. Voskresensky Leonid Gennadievich. |
| Project duration | 01/03/2021 - 31/03/2024 |
| Project’s budget | 200 million VND |
| Classify | Excellent |
| Goal and objectives of the project | - Research and development of new methods for the synthesis of indolysine and indene derivatives.
- Investigation of the biological activities of benzo[h]pyrrolo[2,1-a]isoquinoline derivatives. |
| Main results | - Synthesis of pyrrolo[2,1-a]isoquinoline derivatives by domino reactions of 1-aroyl-substituted 3,4-dihydroisoquinoline with acrylaldehyde has been developed. As the result, four pyrrolo[2,1-a]isoquinoline derivatives (39a-d) have been successfully synthesized in 60% to 91% yields.
- Dihydropyrrolo [2,1-a]isoquinolin-2-yl)methanimine derivatives 40a-b were successfully prepared by the amidation reaction of pyrrolo[2,1-a]isoquinoline 39a-b and 1,4-phenylenediamine. in good yields ranging from 65-70%.
- New approach for the introduction of a perfluoroalkynyl fragment into 1-R2–2-methyl-1,2,3,4-tetrahydroisoquinolines has been developed. Synthesized 1,1-disubstituted isoquinoline compounds under the treatment with
methyl propiolate at 24 ◦C and acetylacetylene at -17 ◦C in trifluoroethanol are converted into 6-perfluoroalkyl substituted allene benzazecines 42a-f and 43a-f in good yields 48-91%.
- Synthesized benzazecines 42a-f and 43a-f were evaluated against four cancer cell lines. Results revealed that compounds 43c and 42b (R2 =Bn, i-Pr; R1 =CF3 displayed good cytotoxic effects on four tested cell lines with IC50 values ranging from 22.14 to 50 μM.
- 01 Article was published on ISI international jounal Journal of Flourine Chemistry.
- Contributed to training 01 bachelor in Chemistry.
Project improved scientific cooperation between Institute of Chemistry and People Friendship University of Russia. |
| Novelty and actuality and scientific meaningfulness of the results | - New approach for the introduction of a perfluoroalkynyl fragment into 1-R2–2-methyl-1,2,3,4-tetrahydroisoquinolines has been developed. Synthesized 1,1-disubstituted isoquinoline compounds under the treatment with |
| Products of the project | - Scientific papers in referred journals: 1 articles in international jounals ISI were published: - Alexander A. Titov, Arina Y. Obydennik, Tatiana N. Borisova, Elena A. Sorokina, Leonid G. Voskressensky, Alexey V. Varlamov, Tuyet Anh Dang Thi, Nhat-Thuy-Giang Le,Tuan Anh Le. Development of new approach for the synthesis of 6-perfluoroalkyl substituted allene benzazecines and study of the nature of properties due to the presence of perfluoroalkyl groups. Journal of Flourine Chemistry 2023, 267, 1110109 (10.1016/j.jfluchem.2023.110109, Q2, ISI, IF = 2.1). |
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