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An efficient and convenient microwave-assisted chemical synthesis of (thio)xanthones with additional in vitro and in silico characterization


Verbanac, Donatella; Jain, Subhash C.; Jain, Nidhi; Chand, Mahesh; Čipčić Paljetak, Hana; Matijašić, Mario; Perić, Mihaela; Stepanić, Višnja; Saso, Luciano
An efficient and convenient microwave-assisted chemical synthesis of (thio)xanthones with additional in vitro and in silico characterization // Bioorganic & medicinal chemistry, 20 (2012), 10; 3180-3185 doi:10.1016/j.bmc.2012.03.074 (međunarodna recenzija, članak, znanstveni)


Naslov
An efficient and convenient microwave-assisted chemical synthesis of (thio)xanthones with additional in vitro and in silico characterization

Autori
Verbanac, Donatella ; Jain, Subhash C. ; Jain, Nidhi ; Chand, Mahesh ; Čipčić Paljetak, Hana ; Matijašić, Mario ; Perić, Mihaela ; Stepanić, Višnja ; Saso, Luciano

Izvornik
Bioorganic & medicinal chemistry (0968-0896) 20 (2012), 10; 3180-3185

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
Xanthones; microwave synthesis; Lewis acid; antibacterial; cytotoxicity

Sažetak
Xanthones and their thio- derivatives are a class of pleiotropic compounds with various reported pharmacological and biological activities. Although these activities are mainly determined in laboratory conditions, the class itself has a great potential to be utilized as promising chemical scaffold for the synthesis of new drug candidates. One of the main obstacles in utilization of these compounds was related to the difficulties in their chemical synthesis. Most of the known methods require two steps, and are limited to specific reagents not applicable to a large number of starting materials. In this paper a new and improved method for chemical synthesis of xanthones is presented. By applying a new procedure, we have successfully obtained these compounds with the desired regioselectivity in a shorter reaction time (50 s) and with better yield (> 80%). Finally, the preliminary in vitro screenings on different bacterial species and cytotoxicity assessment, as well as in silico activity evaluation were performed. The obtained results confirm potential pharmacological use of this class of molecules.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Temeljne medicinske znanosti, Farmacija



POVEZANOST RADA


Projekt / tema
098-0982464-2511 - Epigenetičke i imunomodulatorne promjene u zloćudnim tumorima glave i vrata (Koraljka Gall-Trošelj, )
108-1081874-2419 - Epidemiološka obilježja sistemskog eritemskog lupusa u Hrvatskoj (Nada Čikeš, )

Ustanove
Institut "Ruđer Bošković", Zagreb,
Medicinski fakultet, Zagreb

Časopis indeksira:


  • Current Contents Connect (CCC)
  • Web of Science Core Collection (WoSCC)
    • Science Citation Index Expanded (SCI-EXP)
    • SCI-EXP, SSCI i/ili A&HCI
  • Scopus
  • MEDLINE


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