A series of coumarin-tagged β-lactam triazole hybrids (10a -10o) were synthesized and tested for their cytotoxic activity against MDA-MB-231 (triple negative breast cancer), MCF-7 (estrogen receptor positive breast cancer (ER +)) and A549 (human lung carcinoma) cancer cell lines including one normal cell line, HEK-293 (human embryonic kidney). Two compounds 10b and 10d exhibited substantial cytotoxic effect against MCF-7 cancer cell lines with IC 50 values of 53.55 and 58.62 μM, respectively. More importantly, compounds 10b and 10d were non-cytotoxic against HEK-293 cell lines. Structure-activity relationship (SAR) studies suggested that the nitro and chloro group at the C-3 position of phenyl ring are favorable for anticancer activity, particularly against MCF-7 cell lines. Furthermore, antimicrobial evaluation of these compounds revealed modest inhibition of examined pathogenic strains with compounds 10c and 10i being the most promising antimicrobial agents against Pseudomonas aeruginosa and Candida albicans, respectively.
A series
of 25 conjugates has been synthesized to evaluate their
antiplasmodial potency and cytotoxicity against the chloroquine resistant
(CQR) W2 strain of P. falciparum and Vero kidney
cell lines, respectively. Most of the compounds showed IC50 values in the lower nM range and proved to be many fold more active
than chloroquine (CQ). The studies were extended to decipher modes
of action using techniques including UV–vis absorption, NMR
titrations, and mass spectrometry, and conclusions were strengthened
by docking and density functional theory (DFT) simulations. The most
active compound, with IC50 15 nM and selectivity index
>4000, proved to be an interesting template for antimalarial drug
discovery. To the best of our knowledge this is the first report of
a potent naphthalimide based antiplasmodial conjugate.
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