Project's information

Project's title Synthesis and bioactivity testing of some benzamide derivatives
Project’s code GUST.STS.DDT2020-HH14
Research hosting institution Graduate University of Science and Technology
Project leader’s name Dr. Dinh Thi Cuc
Project duration 01/09/2020 - 30/09/2022
Project’s budget 300 million VND
Classify Fair
Goal and objectives of the project

- Synthesis of benzamide derivatives.
- Testing the biological activity of benzamide derivatives on some human cancer cell lines to find substances with strong antitumor activity.
- Promote publications in domestic and foreign journals on research on benzamide derivatives of Vietnam.

Main results

Theoretical results:
- Successfully synthesized 12 benzamide compounds containing benzothiazole and phenyl amine  moiety, including:
+ 8 new benzamide compounds containing benzothiazole moiety across the amide bridge (36a-d, 38a-d).
+ 4 new benzamide compounds containing phenylamine moiety across the amide bridge (41a-b, 43a-b).
- Has synthesized 4 new amide derivatives 40a-b, 42a-b. These are new derivatives not yet described in the references.
- Has confirmed the structure of 12 newly synthesized compounds by modern spectroscopy methods such as IR, 1H-NMR, 13C-NMR, HRMS spectros.
- The cytotoxic activity of 12 new compounds was tested on two human cancer cell lines, A549 cells (lung cancer) and SW480 cells (colon cancer). The results showed that 2 compounds 36a and 36c were active with IC50 values of 29.49 and 27.59 µM respectively. These are very interesting results, which can serve as a premise to expand the research direction.
Applied results: Twelve benzamide compounds were tested for biological activity and showed promising results.

Novelty and actuality and scientific meaningfulness of the results

- For the first time successfully designed and synthesized 12 new benzamide compounds containing benzothiazole and phenylamine moiety through amide bridges.
- Has synthesized 4 new amide derivatives 40a-b, 42a-b which have not been published in any documents.
- An improved method of synthesizing benzamide derivatives by BOP activator has been proposed instead of using old activators such as DCC or CDI, thereby opening up a new direction for efficient synthesis of these compounds.
- For the first time to evaluate the cytotoxic activity of 12 new compounds on 2 human cancer cell lines, A549 cells (lung cancer) and SW480 cells (colon cancer), in which there are 2 new compounds 36a, 36c with good cytotoxic activity with IC50 values of 29.49 and 27.59 µM respectively.

 

Products of the project

- Scientific papers in referred journals: 02 published articles:
+ Dinh Thi Cuc, Nguyen Thi Hien, Vu Ngoc Doan, Tran Dang Thuan, Dang Thi Tuyet Anh, Nguyen Ha Thanh, Trinh Thu Ha, Nguyen Thi Nga, Nguyen Thi Kim Tuyet, and Phan Van Kiem. Design and Synthesis of New 2-Aminobenzamide Derivatives Containing Benzothiazole and Phenylamine Moiety and Their Cytotoxicity. Natural Product Communications, 2022, Volume 17(7): 1–6. DOI: 10.1177/1934578X221116188
+ Dinh Thi Cuc, Nguyen Thi Hien, Trinh Thu Ha, Tran Dang Thuan, Nguyen Thi Nga, Nguyen Thi Kim Tuyet. Synthesis of 2-aminobenzothiazole hybrids containing 2-aminobenzamide group via amide bridge. Journal of Military Science and Technology, 81, 79-85.

Recommendations

This research direction needs to be further studied to find substances with strong biological activity towards the goal of clinical trials and drug development.

Images of project
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