04. Trường Đại học Khoa học tự nhiên (University of Science)
Tài nguyên nội sinh
Các bộ sưu tập số Luận văn Thạc sĩ, Luận án Tiến sĩ, Đề tài Báo cáo khoa học… của Thư viện Trường ĐH. Khoa học tự nhiên – ĐHQG-HCM được xây dựng nhằm hỗ trợ cho hoạt động giảng dạy và nghiên cứu của Nhà trường.
Duyệt 04. Trường Đại học Khoa học tự nhiên (University of Science) theo Chủ đề "4--aza-2,3-didehydropodophyllotoxins"
- Ấn phẩmSynthesis and cytotoxicity of new 4-aza-2,3-didehydropodophyllotoxins(Viện Kỹ thuật Nhiệt đới, Viện Hàn lâm Khoa học và Công nghệ Việt Nam, 2022-02) Nguyen, Thi Thuy Hang; Tran, Thi Yen; Vu, Dinh Hoang; Ngo, Quoc AnhPodophyllotoxin is a lignan, first isolated from herbaceous plants of Podophyllum and possess a potent antiviral and antitumor agent. Podophyllotoxin and its analogs exhibit antineoplastic activities mainly by preventing the assembly of tubulin into microtubules or inhibiting the catalytic activity of DNA topoisomerase II. Recently, many series of novel conjugates of 4-aza-2,3-didehydropodophyllotoxin analogs were synthesized and demonstrated significant cytotoxicity. Some compounds inhibit tubulin polymerization comparable to podophyllotoxin. These compounds were also shown to arrest the cell cycle in the G2/M phase of cell cycle and to lead to caspase-3 dependent apoptotic cell death. In this paper, we report the synthesis of five new 4-aza-2,3-didehydropodophyllotoxins by a straightforward multicomponent reaction in the hope of finding new structures with interesting anticancer activity. The novelty in our work is the preparation of quinoline structural compounds of podophyllotoxin derivatives, in two simple steps, having functional groups which are available for further modifications. The “one-pot” synthesis process increased performance as well as minimized the steps involved. The obtained compounds with podophyllotoxin frame have the corresponding yields of 60 - 83 %. Five new 4-aza-2,3-didehydropodophyllotoxins demonstrated comparable cytotoxicity against the Hep-G2, MCF7 cell lines with an IC50 value of 52.2 - 261.2 µM, and with ellipsitine as the positive control.