Novel 6,7,8-trihydrobenzo[6',7']cyclohepta[2',1'-e]pyrazolo[2,3-a]pyrimidine derivatives as Topo IIα inhibitors with potential cytotoxic activity

Autor:	Thoraya A. Farghaly, Hanan Gaber Abdulwahab, Hanadi Y. Medrasi, Mariam A. Al-sheikh, Dina F. Katowah, Amani M.R. Alsaedi
Rok vydání:	2022
Předmět:	Dose-Response Relationship Drug Molecular Structure Organic Chemistry Antineoplastic Agents Biochemistry Molecular Docking Simulation Structure-Activity Relationship Pyrimidines Doxorubicin Cell Line Tumor Drug Discovery Drug Screening Assays Antitumor Molecular Biology Cell Proliferation
Zdroj:	Bioorganic Chemistry. 128:106043
ISSN:	0045-2068
DOI:	10.1016/j.bioorg.2022.106043
Popis:	Novel tetracyclic pyrazolo[1,5-a]pyrimidine derivatives; namely benzo[3,4]cyclohepta[1,2-e]pyrazolo[1,5-a]pyrimidin-2-amines 6a-e and benzo[3,4]cyclohepta[1,2-e]pyrazolo[1,5-a]pyrimidin-2(6H)-ones 15a-d, were designed and synthesized as topoisomerase IIα inhibitors with potential anticancer activity. The structure and their mechanistic pathway were discussed and confirmed based on spectral data and DFT calculations. Compounds 6a, 6c, 15b, 15c and 15d exhibited potent Topo II inhibitory activity at one-digit IC
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::04452c5d78c5601e7535e1d5b903c262 https://doi.org/10.1016/j.bioorg.2022.106043 Zobrazit plný text záznamu Full Text from ScienceDirect