2. Academic Validation
  3. Synthesis and biological evaluation of novel benzo[a]pyridazino[3,4-c]phenazine derivatives

Synthesis and biological evaluation of novel benzo[a]pyridazino[3,4-c]phenazine derivatives

  • Bioorg Med Chem Lett. 2021 Jul 1:43:128054. doi: 10.1016/j.bmcl.2021.128054.
Giang Le-Nhat-Thuy 1,  Tuyet Anh Dang Thi 2,  Quynh Giang Nguyen Thi 2,  Phuong Hoang Thi 3,  Tuan Anh Nguyen 3,  Ha Thanh Nguyen 3,  Thu Ha Nguyen Thi 3,  Hoang Sa Nguyen 4,  Tuyen Van Nguyen 5
Affiliations

Affiliations

  • 1 Institute of Chemistry, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam; Graduate University of Science and Technology, VAST, 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam. Electronic address: lenhatthuygiang@yahoo.com.
  • 2 Institute of Chemistry, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam; Graduate University of Science and Technology, VAST, 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam.
  • 3 Institute of Chemistry, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam.
  • 4 University of Khanh Hoa, 1 Nguyen Chanh, Nhatrang, Khanhhoa, Viet Nam.
  • 5 Institute of Chemistry, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam; Graduate University of Science and Technology, VAST, 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam. Electronic address: ngvtuyen@hotmail.com.
PMID: 33895275 DOI: 10.1016/j.bmcl.2021.128054
Abstract

A convenient microwave-assisted one-pot four-component synthetic approach was developed en route to novel functionalized benzo[a]pyridazino[3,4-c]phenazine derivatives starting from 2-hydroxy-1,4-naphthoquinone, aromatic aldehydes, methyl hydrazine and o-phenylenediamine. Nine new derivatives were successfully synthesized and subsequently evaluated in terms of their biological profiles. The results revealed good cytotoxic activities of compounds 6a, 6h against KB, HepG2, Lu1 and MCF7 human Cancer cell lines. Besides that, compound 6d exhibited promising antimicrobial activities toward Staphylococcuc aureus and Bacillus subtilis Bacterial strains with IC50 < 6 μM.

Keywords

2-Hydroxy-1,4-naphthoquinone; 4-c]Phenazines; Antimicrobial activity; Benzo[a]pyridazino[3,4-c]phenazines; Cytotoxicity; Multicomponent reactions.

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