High in vitro

The 6- uoro isomers, 6-deoxy-6-demethyl-6a- uorotetracycline [24333-20-8] C2 H2 FN20y, and 6-deoxy-6-demethyl-6P- uorotetracycline [24333-21-9] C2 H2 FN202, have been prepared and showed relatively high in vitro and in vivo biological activities compared to the parent tetracyclines. 

There is no meaningflil correlation between laboratory corrosion tests and clinical performance, but high in vitro corrosion rates on several high nickel dental prosthetic alloys (163), together with the prevalence of allergy to nickel caused by plated jewelry, gives cause for caution. 

When reacted with tetraalkylammonium halides, hydrated [Me2Sn(IV)], [Bu2Sn(IV)]2-",2 [Ph2Sn(IV)]2-", 5 and [EtPhSn(lV)]2-",2 ester derivatives of 2,6-pyridinedicarboxylic acid yield tetraalkylammonium diorganohalogeno(2,6-pyr-idinedicarboxylato)stannates. Both classes of compounds exhibit high in vitro antitumor activity. 

DiMaio J, Schiller PW. A cyclic enkephalin analog with high in vitro opiate activity. Proc Natl Acad Sci USA 1980 77 7162-7166. 

The pyridazino[6,l-A quinazoline 114 (Ar = 4-biphenyl) exhibited high in vitro antibacterial activity against Staphylococcus aureus and anifungal activity against Aspergillus fumigatus <2001RRC649>. 

With the introduction of chlorpromazine in 1952, there was a small revolution in psychiatry patients suffering from psychosis were able to be de-institutionalized. Chlorpromazine and other typical antipsychotics (e.g., haloperidol) demonstrate high in vitro binding affinities for the dopamine D2 receptor (D2). Specifically, their... 

To determine if the high in vitro potents of the anti-HIV compound 30 translates into antiviral efficiency in vivo, Datema et al. investigated the inhibition of HIV-1 production and of depletion of human T cells in HIV-1-infected SCID-hu Thy/Liv mice [37]. Steady levels of 100 ng of 30 or higher per mL in plasma resulted in significant inhibition of HIV p24 protein formation. Daily injection of 30 caused a dose-dependent decrease in viral p24 production, and this inhibition could be potentiated by coadministration of AZT (or DDI). This study suggested that 30 alone or in combination with the licensed anti-HIV agents AZT and DDI may decrease the virus load in HIV-infected patients and, by extension, that the infectious cell entry step is a valid target for antiviral chemotherapy of HIV disease. 

The high in vitro activity of the inhibitors often does not translate into valuable antibiotic activity because of the combination of poor cell penetration and lack of selectivity. 5 -0-[A-(Aminoacyl)sulfamoyl] adenosines are potent inhibitors of aaRS, but their whole-cell antibacterial activity is very limited. 5 -0-[N-(Dipeptidyl)sulfamoyl] adenosines (Figure 15) showed improved antibacterial activity. ° These compounds can be regarded as synthetic analogues of the natural product microcin C (18) (Figure 13). 

Escherichia coli Synthetic HRP C gene under control of the tac promoter. High In vitro refolding required to obtain active enzyme yield 2—i mg liter" (64, 68). Higher yields reported (69, 70). 

Rifamycin SV (133, Fig. 23) is a naturally occurring macrocycle isolated from Nocardia mediterranei by Senti, Greco and Ballotta in 1959. It shows a high in vitro antibiotic activity through inhibition of DNA-dependent RNA polymerase, but bioavailability is low due to its poor water solubility. The semisynthetic derivative rifampicin (135) displays markedly higher water solubility and in vivo activity. We chose 3-formylrifamycin (134) as model macrocycle for the possibility of binding it to solid phase by hydrazone bond formation in a manner similar to rifampicin (Fig. 24). 

The symmetrical seven-membered sulfone, 11 (Table I), has been reported by Kim to show high in vitro potency (IC50 = 1 nM), good antiviral activity in cell culture (EC90 = 20 nJM), and excellent pharma-... 

Fig. 7 Examples of ruthenium(II)-arene and osmium(II)-arene paullone complexes with high in vitro anticancer activity...

Dinuclear Ru-arene, complexes based on maltol-derived ligands with a varying spacer length (Fig. 9) were shown to exhibit high in vitro anticancer activity [64,65], whereas the mononuclear analogue was inactive [66]. In another approach, two organometallic Ru-arene moieties were linked via a ferrocene unit (Fig. 10)... 

NH2)]+ [X is OH2 (84a), THP (85a)] conjugates were also prepared (Scheme 21). These complexes retain high in vitro and in vivo specificity for the... 

The 18F-containing steroid 328 exhibits high in vitro GR (glucocorticoid receptor) binding affinity318. 

Cyclopent[b]indolequinones, (I), another new class of reductive alkylating agent having high in vitro cytotoxicity and antitumor activity, were prepared by the authors... 

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