Antihuman Immunodeficiency Virus Type 1 (HIV‐1) Activity of Rare Earth Metal Complexes of 4‐Hydroxycoumarins in Cell Culture

Abstract

The cerium , lanthanum , and neodymium complexes with 4-hydroxy-3-(3-oxo-1-phenylbutyl)-2H-1-benzopyran-2-one (warfarin) (W) and 3,3′-benzylidenebis[4-hydroxycoumarin] (1) were synthesized and studied for the first time for cytotoxicity (on MT-2 cells) and as anti-HIV agents under acute and chronic infection. The complexes were characterized by different physicochemical methods: mass spectrometry, NMR, NMR, and IR spectroscopy. The spectra of the complexes were interpreted on the basis of comparison with the spectrum of the free ligands. Anti-HIV effect of the complexes/ligands was measured in MT-2 cells by microtiter infection assay. Detection of endogenous reverse transcriptase (RT) activity and RT processivity by PCR indicative for proviral DNA synthesis demonstrated that anti-HIV activity has not been linked to early stages of viral replication. No effect on late steps of viral replication has been found using cells chronically producing HIV-1LAI virus. demonstrated anti-HIV activity (IC50=21.4 μM) close to maximal nontoxic concentration. , , and demonstrated limited anti-HIV potency, so none of the complexes seems appropriate to be used in clinic. Further targeting of HIV-1 inhibition by is under progress.

In-vitro antibacterial, antifungal activity of some transition metal complexes of thiosemicarbazone Schiff base (HL) derived from N4-(7′-chloroquinolin-4′-ylamino) thiosemicarbazide

“…The new bands observed in the regions 560-540, 460-445 and 365-355 cm 21 are tentatively assigned to n(M-O), n(M-N) and n(M-S) (metal-ligand) stretching bands, respectively [34].…”

“…The strong band observed at 876 cm 21 in the spectrum of HL, is mainly due to the stretching vibrations of (CvS), is shifted towards lower frequency and occurred at 850-820 cm 21 . in the corresponding spectra of the metal complexes indicating the coordination of the thio-keto sulphur to metal atom [34].…”

“…The proton peak of NZH group at d 2.4 and 11.67 ppm remains the same in the ligand, and in the complexes it suggested that deprotonation do not occur and it has also shown keto form of the ligand. The signal due to the SZH (thiol) is not observed in the expected range 2-3 ppm [34,40] indicating that the ligand exist in the thione form. The multiplets as strong bands in region d 7.7-8.24 ppm were assigned to aromatic and quinoline ring protons, which also shifted down field in the complexes.…”

Synthesis and electrochemical study of new 3-(hydroxyphenyl)benzo[f]coumarins

“…Coumarins are also described as antiviral, vasorelaxant, antioxidant, antimicrobial, anticancer, anti-inflammatory and enzymatic inhibitors [22][23][24][25][26][27][28][29][30][31][32][33], but limited data is available concerning their antioxidant activity [22,30,[34][35][36].…”

Synthesis, Structure, Protolytic Properties, Alkylating and Cytotoxic Activity of Novel Platinum(II) and Palladium(II) Complexes with Pyrazole‐Derived Ligands

“…[39,40] The rare earth metal complexes of coumarin derivatives endowed with anticoagulant and anti-HIV activity were also documented. [41][42][43] Current efforts are focused on developing metalbased drugs with improved clinical effectiveness, reduced general toxicity and a broader spectrum of activity.…”