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Synthesis, Characterization, Bioactivity, and POM Analyses Of Isothiochromeno[3,4-E][1,2]Oxazines

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Wed, 2013-03-13 15:32 — Ismail Warad
Journal Title, Volume, Page: 
Medicinal Chemistry Research October 2013, 22, 4798-4809
Year of Publication: 
2013
Link: 
http://link.springer.com/article/10.1007/s00044-012-0392-4
Authors: 
Brahim Bennani
Laboratoire de Chimie Organique, Faculté desz Sciences Dhar El-Mehraz, Université Sidi Mohammed Ben Abdellah, 30000, Fez, Morocco
Abdelali Kerbal
Laboratoire de Chimie Organique, Faculté desz Sciences Dhar El-Mehraz, Université Sidi Mohammed Ben Abdellah, 30000, Fez, Morocco
Bouchra F. Baba
Laboratoire de Chimie Organique, Faculté desz Sciences Dhar El-Mehraz, Université Sidi Mohammed Ben Abdellah, 30000, Fez, Morocco
Maria Daoudi
Laboratoire de Chimie Organique, Faculté desz Sciences Dhar El-Mehraz, Université Sidi Mohammed Ben Abdellah, 30000, Fez, Morocco
Ismail Warad
Department of Chemistry, Science College, King Saud University, P.O. Box 2455, Riyadh, 11451, Saudi Arabia
Current Affiliation: 
Department of Chemistry, Faculty of Science, An-Najah National University, Nablus, Palestine
[email protected]
Mohamad Aljofan
Department of Microbiology, School of Medicine, Nursing and Health Sciences, Monash University, Caulfield East, VIC, Australia
Ahmed M. Alafeefy
Department of Pharmaceutical Chemistry, College of Pharmacy, Salman Bin Abdulaziz University, P.O. Box 173, Alkharj, 11942, Saudi Arabia
Vijay Masand
Department of Chemistry, Vidya Bharati College, Camp, Amravati, Maharashtra, India
Taibi B. Hadda
Laboratoire Chimie des Matériaux, Faculté des Sciences d’Oujda, Université Mohammed Premier, 60000, Oujda, Morocco
[email protected]
Preferred Abstract (Original): 
A series of 18 new 3,4-disubstituted-isothiochromeno[3,4-e][1,2]oxazines 28–45 has been obtained from the 3′,4′-di-substituted-4′H-spiro[isothiochromene-3,5′-isoxazol]-4(1H)-ones 10–27 in refluxing HCl acid/ethanol. A series of 15/18 compounds 28–45 was selected by the National Cancer Institute (NCI, Bethesda, USA) and were evaluated against a full panel of 60 primary human tumor cell lines derived from nine human cancer types, all of which showed antiproliferative activity in the micromolar range. The most active compound number 37 (S722910) showed high potency against all the tested cell lines with a GI50 mean value in the range of 30–80 μM; TGI and LC50 values were 12–16 μM having positive response on 98 and 63 % of the tested cell lines (Breast-MCF7 and NCS-SF-268) respectively.