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Antitumor and antileishmanial evaluation of novel heterocycles derived from quinazoline scaffold: a molecular modeling approach

Medicinal Chemistry Research(2012)

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摘要
Novel thiazole, pyrimidine and benzylidene derivatives derived from quinazoline scaffold have been synthesized. The antitumor evaluation of the newly synthesized products against three cancer cell lines namely breast adenocarcinoma (MCF-7), non-small cell lung cancer (NCI-H460), and CNS cancer (SF-268) showed that the benzylidene–quinazoline derivative 12a showed remarkable activity against all three cell lines. The thiazolo-quinazoline derivative 10 showed greater activity than the control against breast adenocarcinoma (MCF-7) with a concentration of 0.01 μM. Moreover, the antileishmanial activity of the newly synthesized products tested on Leishmania donovani amastigotes showed that compounds 4, 14, and 18 had very promising activity.
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关键词
Quinazolines, Thiazole, Pyrimidine, Antitumor, Antileishmanial
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