Antimalarial, antimycobacterial and antiproliferative activity of phenyl substituted mixed tetraoxanes | Zendy

Dejan Opsenica | Zendy; Dennis E. Kyle | Zendy; Milhous Wilbur | Zendy; Bogdan A. Šolaja | Zendy

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Antimalarial, antimycobacterial and antiproliferative activity of phenyl substituted mixed tetraoxanes

Author(s) -

Dejan Opsenica,

Dennis E. Kyle,

Milhous Wilbur,

Bogdan A. Šolaja

Publication year - 2003

Publication title -

journal of the serbian chemical society

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.227

H-Index - 45

eISSN - 1820-7421

pISSN - 0352-5139

DOI - 10.2298/jsc0305291o

Subject(s) - antimycobacterial , artemisinin , amide , chemistry , plasmodium falciparum , in vitro , stereochemistry , combinatorial chemistry , solid tumor , paclitaxel , pharmacology , malaria , tuberculosis , organic chemistry , mycobacterium tuberculosis , biology , medicine , biochemistry , chemotherapy , immunology , cancer , pathology

Mixed tetraoxanes of the 4"-phenyl-substituted cyclohexyl-spirotetraoxacyclo- hexyl-spirocholate series have been prepared and evaluated as possible antimalarials, anti- proliferatives and antimycobacterials. The activity of the (4"R or S)-phenyl series against P. falciparum D6 and W2 strains was found to be at the level of artemisinin, with two com- pounds, the acid 4 and the amide 6, exhibiting encouraging anti-TB activity as well. Very promising in vitro results of the said tetraoxanes were obtained against solid tumours and, in some instances, the activity against a selected number of cell lines was higher than that of the antitumor drug paclitaxel.

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