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Abstract:
Azamacrocyclic fluorophores containing piperazine units were synthesized
using sequential rhodium-catalyzed regioselective hyd
Several cis and trans bis-steroidal 1,2,4,5-tetraoxanes possessing amide terminus were synthesised and evaluated as antimalarials
and antiproliferatives. The compounds exhibited submicromolar antimalarial
activity against Plasmodium falciparum D6 and W2
strains. The existence of HNC(O) moiety was found
necessary for pronounced antimalarial and antiproliferative activity. In antiproliferative
screen, the trans tetraoxane
6 was found to exhibit a pronounced cytotoxicity on
14 cancer cell lines. In addition, tetraoxanes 11 and
12 exhibited significant cytotoxic activity too; microscopic
examination of treated HeLa cells showed
morphological appearance reminiscent for apoptosis (condensed and/or fragmented
nuclei).
