Affiliation:
1. State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization Xinjiang Technical Institute of Physics and Chemistry Chinese Academy of Sciences South Beijing Rd 40–1 Urumqi 830011 P. R. China
2. University of Chinese Academy of Sciences 19 A Yuquan Rd Beijing 100049 P. R. China
3. Faculty of Chemistry Samarkand State University University Blvd. 15 Samarkand 140104 Uzbekistan
4. Urgench State University Kh. Olimjon st. 14 Urgench 220100 Uzbekistan
Abstract
AbstractThe chemical transformation of the tricyclic furo[2,3‐d]pyrimidines was performed under isosteric and scaffold‐hopping strategies focusing on the synthesis of its arylidene and imine‐containing derivatives. Naturally‐occurring alkaloids mackinazolinone and isaindigotone were as templates of target heterocycles. Synthesized compounds evaluated for their antitumor activity on human cancer cervical HeLa, breast MCF‐7, and colon HT‐29 cell lines. Four compounds: 8c, 8e, 10b, and 10c demonstrated potency against HeLa and HT‐29 cell lines, and IC50 values were between 7.37–13.72 μM, respectively. The molecular docking results showed that compounds 8c and 10b had good binding and high matching with the target EGFR protein.
Funder
National Key Research and Development Program of China
Subject
Molecular Biology,Molecular Medicine,General Chemistry,Biochemistry,General Medicine,Bioengineering
Cited by
5 articles.
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