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In vitro antitumor and antiviral activities of new benzothiazole and 1,3,4-oxadiazole-2-thione derivatives
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In vitro antitumor and antiviral activities of new benzothiazole and 1,3,4-oxadiazole-2-thione derivatives
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Journal Article
In vitro antitumor and antiviral activities of new benzothiazole and 1,3,4-oxadiazole-2-thione derivatives
2008
Overview
A series of new benzothiazole derivatives 6a-h have been synthesized, in five steps, from substituted phenols via the 1,3,4-oxadiazole-2-thiones 5a-h. The in vitro antitumor activity of the compounds obtained was investigated and the benzothiazol derivatives 6d and 6e showed strong effects on leukaemia cell lines CCRF-CEM (CC50 = 12 ± 2 μmol L-1, 8 ± 1 μmol L-1, respectively). These compounds are leading candidates for further development. The title compounds were tested against representatives of several virus families containing single stranded RNA genomes, either positive-sense (ssRNA+), or negativesense (RNA-), and against double-stranded RNA genomes (dsRNA), as well as some Flaviviridae viruses.
U pet reakcijskih koraka sintetizirana je serija novih derivata benzotiazola 6a-h polazeći iz supstituiranih fenola preko 1,3,4-oksadiazol-2-tiona 5a-h. Sintetizirani spojevi ispitani su na antitumorsko djelovanje. Benzotiazol derivati 6d i 6e pokazali su jak učinak na staničnu liniju leukemije CCRF-CEM (CC50 = 12 ± 2, odnosno 8 ± 1 μmol L-1). Ti su spojevi predvodni spojevi za daljnji razvoj. Nadalje, novi su spojevi testirani na djelovanje na nekoliko tipova virusa koji sadrže bilo pozitivni (ssRNA+) bilo negativni (RNA-) jednolančani RNA genom ili dvolančani RNA genom (dsRNA), te na neke Flaviviridae viruse.
Publisher
Versita,De Gruyter Brill Sp. z o.o., Paradigm Publishing Services
Subject
/ Animals
/ Antineoplastic Agents - chemical synthesis
/ Antineoplastic Agents - pharmacology
/ Antiviral Agents - chemical synthesis
/ Antiviral Agents - pharmacology
/ Benzothiazoles - chemical synthesis
/ Benzothiazoles - pharmacology
/ Cell Survival - drug effects
/ Cytopathogenic Effect, Viral - drug effects
/ Dose-Response Relationship, Drug
/ Humans
/ Oxadiazoles - chemical synthesis
/ Structure-Activity Relationship
