An efficient synthesis of several N-[(1-benzyl-1,2,3-triazol-4-yl)methyl]carboxamides in the 13b-and 13a-D-secoestrone series is reported. Novel triazoles were synthesized via the Cu(I)-catalyzed azide-alkyne cycloaddition of steroidal alkynyl carboxamides and p-substituted benzyl azides. Each of the products was evaluated in vitro by means of MTT assays for antiproliferative activity against a panel of human adherent cancer cell lines (HeLa, MCF-7, A431 and A2780). Some of them exhibited activities similar to those of the reference agent cisplatin. On change of the substitution pattern of the benzyl group of the azide, great differences in the cell growth-inhibitory properties were observed. The p-alkylbenzyl-substituted triazoles selectively exerted high cytostatic action against A2780 cells, with IC 50 values of 1 mM. We investigated the potential inhibitory action exerted on the human 17b-HSD1 activity of the new secosteroids. Three triazoles effectively suppressed the estrone to 17b-estradiol conversion with IC 50 values in low micromolar range.

Biological control against microbial infections has a great potential as an alternative approach instead of fungicidal chemicals, which can cause environmental pollution. The pigment producer Metschnikowia andauensis belongs to the antagonistic yeasts, but details of the mechanism by which it inhibits growth of other microbes are less known. Our results confirmed its antagonistic capacity on other yeast species isolated from fruits or flowers and demonstrated that the antagonistic capacity was well correlated with the size of the red pigmented zone. We have isolated and characterized its red pigment, which proved to be the iron chelating pulcherrimin. Its production was possible even in the presence of 0.05 mg/ml copper sulphate, which is widely used in organic vineyards because of its antimicrobial properties. Production and localisation of the pulcherrimin strongly depended on composition of the media and other culture factors. Glucose, galactose, disaccharides and the presence of pectin or certain amino acids clearly promoted pigment production. Higher temperatures and iron concentration decreased the diameter of red pigmented zones. The effect of pH on pigment production varied depending of whether it was tested in liquid or solid media. In addition, our results suggest that other mechanisms besides the iron depletion of the culture media may contribute to the antagonistic capacity of M. andauensis.

U b e r d i e E r f i i U b a r k e i t d e~j e n i g e n Z~h l a u s d r f i c k e , w e l c h e i n d e r N o r m a l f o r m z w e i b e n a c h b a r t e A l l z e i e h e n e n t h a l t e n . Von L~szl6 K a l m s in Szeged (Ungarn).Einleitung.

In the first paper of the above main title, one of us has proved that any formula of the first order predicate calculus is equivalent (as to being satisfiable or not) to some binary first order formula having a prefix of the form (Ex1)(x2)(Ex3) … (xn) and containing a single predicate variable. This result is an improvement of a theorem of Ackermann stating that any first order formula is equivalent to another with a prefix of the above form but saying nothing about the number of predicate variables appearing therein. Hence the question arises if other theorems reducing the decision problem to the satisfiability question of the first order formulas with a prefix of a special form can be improved in like manner. In the present paper we shall answer this question concerning Gödel's reduction theorem stating that any first order formula is equivalent to another the prefix of which has the form

1. Although the decision problem of the first order predicate calculus has been proved by Church to be unsolvable by any (general) recursive process, perhaps it is not superfluous to investigate the possible reductions of the general problem to simple special cases of it. Indeed, the situation after Church's discovery seems to be analogous to that in algebra after the Ruffini-Abel theorem; and investigations on the reduction of the decision problem might prepare the way for a theory in logic, analogous to that of Galois.It has been proved by Ackermann that any first order formula is equivalent to another having a prefix of the form(1) (Ex1)(x2)(Ex3)(x4)…(xm).On the other hand, I have proved that any first order formula is equivalent to some first order formula containing a single, binary, predicate variable. In the present paper, I shall show that both results can be combined; more explicitly, I shall prove theTheorem. To any given first order formula it is possible to construct an equivalent one with a prefix of the form (1) and a matrix containing no other predicate variable than a single binary one.2. Of course, this theorem cannot be proved by a mere application of the Ackermann reduction method and mine, one after the other. Indeed, Ackermann's method requires the introduction of three auxiliary predicate variables, two of them being ternary variables; on the other hand, my reduction process leads to a more complicated prefix, viz.,(2) (Ex1)…(Exm)(xm+1)(xm+2)(Exm+3)(Exm+4).

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Experiments reported here were designed to investigate the effect of silibinin (extracted from Silybum marianum) on human polymorphonuclear leukocyte (PMN) motility and on leukocyte immobilizing activity of lymphokine (leukocyte inhibitory factor, LIF), formyl-Met-Leu-Phe (fMLP), calcium ionophore A-23187 and human sera inactivated by heat (HI-S). In the in vitro experiments, silibinin (1-10 micrograms/ml) failed to influence the random motility of unstimulated PMNS in agarose droplet assay, but enhanced the motility of the PMNs immobilized by fMLP, calcium ionophore, LIF or by autologous human sera. In the in vivo study, silibinin (Legalon-70) two hours after the administration was effective in enhancing spontaneous motility of leukocytes obtained from health volunteers which action could be regarded as a consequence of the decrease of leukocyte immobilizing activity being present in normal human plasma.