Synthesis of 2,4-diaryl chromenopyridines and evaluation of their topoisomerase I and II inhibitory activity, cytotoxicity, and structure–activity relationship

Autor:	Eunyoung Lee, Won-Jea Cho, Pritam Thapa, Yurngdong Jahng, Eung-Seok Lee, Jae Hun Choi, Uttam Thapa, Younghwa Na, Kyung Hwa Jeon, Youngjoo Kwon, Minho Yun, Radha Karki, Eun Mi Ha
Rok vydání:	2011
Předmět:	Male Pyridines Stereochemistry Antineoplastic Agents Chemical synthesis Structure-Activity Relationship chemistry.chemical_compound Antigens Neoplasm Cell Line Tumor Neoplasms Drug Discovery Humans Topoisomerase II Inhibitors Structure–activity relationship Benzopyrans Cytotoxicity Cell Proliferation Pharmacology chemistry.chemical_classification biology Topoisomerase Organic Chemistry General Medicine DNA-Binding Proteins DNA Topoisomerases Type II Enzyme DNA Topoisomerases Type I chemistry Cell culture Enzyme inhibitor biology.protein Female Drug Screening Assays Antitumor Topoisomerase I Inhibitors Terpyridine
Zdroj:	European Journal of Medicinal Chemistry. 46:3201-3209
ISSN:	0223-5234
Popis:	Designed and synthesized were a series of 5 H -chromeno[4,3- b ]pyridines with substitution at 2- and 4-positions with various 5- or 6-membered heteroaromatics as antitumor agents. They were evaluated for topoisomerase I and II inhibitory activities as well as cytotoxicities against several human cancer cell lines. Structure–activity relationship study showed that 2-furyl or 2-thienyl at 2- or 4-position of central pyridine is crucial in displaying topo I or II inhibitory activity and cytotoxicity.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1eada9df14b973a1131b3a28b62d302f https://doi.org/10.1016/j.ejmech.2011.04.029 Zobrazit plný text záznamu Full Text from ScienceDirect