GET THE APP

Synthesis, Characterization, and In vitro Anticancer Evaluation of 7-Piperazin-Substituted [1,3]Oxazolo[4,5-D]Pyrimidines | Abstract

Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry

ISSN: 0975-413X
All submissions of the EM system will be redirected to Online Manuscript Submission System. Authors are requested to submit articles directly to Online Manuscript Submission Systemof respective journal.

Abstract

Synthesis, Characterization, and In vitro Anticancer Evaluation of 7-Piperazin-Substituted [1,3]Oxazolo[4,5-D]Pyrimidines

Author(s): Yevgeniya S Velihina, Maryna V Kachaeva, Stepan G Pilyo, Victor V Zhirnov, Volodymyr S Brovarets

A novel series of five 7-piperazin-substituted [1,3]oxazolo[4,5-d]pyrimidines have been synthesized and characterized by Infrared (IR), Proton Nuclear Magnetic Resonance (1H-NMR), Carbon-13 Nuclear Magnetic Resonance (13C-NMR) spectroscopy, elemental analysis and chromato-mass-spectrometry. The anticancer activities of the all the newly synthesized compounds were valuated via single high dose (10-5M) against 60 cancer cell lines by the National Cancer Institute according to its own screening protocol. In the next phase, the compounds have been selected for five-dose assay. Among these compounds 5-phenyl-7-piperazin-1-yl-2-p-tolyl[1,3]oxazolo[4,5-d]pyrimidine displayed the most growth inhibitory (GI50 was in range of 0.2−2.0 μM), cytostatic (TGI − 0.3-4.2 μM) and cytotoxic (LC50 − 0.6-7.8 μM with the exception of Leukemia CCRF-CEM cell line, LC50>100 μM) activities against all cancer cell lines. The most selectivity 5-phenyl-7-piperazin-1-yl-2-p-tolyl[1,3]oxazolo[4,5-d]pyrimidine demonstrated against Leukemia and Colon Cancer subpanels. These results provided evidence that compound could be useful for developing new anticancer drugs.


Full-Text PDF

Select your language of interest to view the total content in your interested language

30+ Million Readerbase
SCImago Journal & Country Rank
Google Scholar citation report
Citations : 23677

Der Pharma Chemica received 23677 citations as per Google Scholar report

Der Pharma Chemica peer review process verified at publons
Der Pharma Chemica- Journals on pharmaceutical chemistry