Synthesis and cytotoxicity  of new 4-aza-2,3-didehydropodophyllotoxins

Nguyen Thi Thuy Hang; Tran Thi Yen; Vu Dinh Hoang; Ngo Quoc Anh

doi:10.15625/2525-2518/15577

Author affiliations

Authors

Nguyen Thi Thuy Hang Institute of Chemistry, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Cau Giay, Ha Noi, Viet Nam
Tran Thi Yen Institute of Chemistry, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Cau Giay, Ha Noi, Viet Nam
Vu Dinh Hoang Department of Pharmaceutical Chemistry, Hanoi University of Science and Technology, 1 Dai Co Viet, Bach Khoa, Hai Ba Trung, Ha Noi, Viet Nam
Ngo Quoc Anh Institute of Chemistry, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Cau Giay, Ha Noi, Viet Nam

DOI:

https://doi.org/10.15625/2525-2518/15577

Keywords:

quinolin, podophyllotoxin, one-pot, cytotoxiccity

Abstract

Five new 4-aza-2,3-didehydropodophyllotoxins were synthesized by a straightforward multi-component reaction in the hope of finding new structures with interesting anticancer activity. The “one-pot” synthesis process is developed to increase performance as well as minimize 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, MCF7cell lines with an IC₅₀ value of 52.2 - 261.2 µM with ellipsitine as the positive control.

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