Open AccessDesign and Synthesis of 4-O-Podophyllotoxin Sulfamate Derivatives as Potential Cytotoxic Agents
Author(s) -
Ammar Bader,
Majdi M. Bkhaitan,
Ashraf N. Abdalla,
Qasem Abdallah,
Hamed I. Ali,
Dima A. Sabbah,
Ghadeer Albadawi,
Ghassan Abushaikha
Publication year - 2021
Publication title -
evidence-based complementary and alternative medicine
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.552
H-Index - 90
eISSN - 1741-4288
pISSN - 1741-427X
DOI - 10.1155/2021/6672807
Subject(s) - podophyllotoxin , chemistry , cytotoxicity , lignan , etoposide , cell culture , allium , cytotoxic t cell , selectivity , apoptosis , pharmacology , biochemistry , stereochemistry , combinatorial chemistry , in vitro , biology , chemotherapy , medicine , botany , genetics , catalysis
4-O-Podophyllotoxin sulfamate derivatives were prepared using the natural lignan podophyllotoxin. The prepared compounds were afforded by reacting O-sulfonyl chloride podophyllotoxin with ammonia or aminoaryl/heteroaryl motif. Biological evaluation was performed in human breast cancer (MCF7), ovarian cancer (A2780), colon adenocarcinoma (HT29), and normal lung fibroblast (MRC5) cell lines. Compound 3 exhibited potent inhibitory activity and good selectivity margin. Compounds 2 , 3, and 7 exerted apoptotic effect in MCF7 cells in a dose-dependent manner. The cytotoxicity of the verified compounds was inferior to that of podophyllotoxin.