Cytotoxic and antitumor activity of a new series of heterocyclic compounds: dipyrido (4,3-b) (3,4-f) indoles]

Among newly synthesized compounds derived from the dipyrido [4,3-b] [3,4-f] indole nucleus, two have proved to be particularly active in vitro and in vivo. Their cytotoxic effects on cultured cells have been determined. At non toxic doses, they displayed a pronounced inhibitory effect on experimental L1210 Leukemia. These compounds have a strong affinity for DNA molecules.     

Some relations between the structure and the antibacterial activity of natural coumarins

Zusammenfassung Von 15 untersuchten natürlichen Cumarinen und Furocumarinen besitzen Ammoresinol und Ostruthin stärkste Wirkung auf Gram-positive Mikroorganismen. Zur Ammoresinolwirkung ist die Erhaltung der freien -OH-Gruppen notwendig, während bei Ostruthin durch Vitamin K₂ die Wirksamkeit vermindert wird.     

Conformations and biological properties of apomorphine and its phenanthro(10,1-b,c)azepine homologue.

11,12-Dihydroxy-7-methyl-4,5,6,7,7a,8-hexahydrophenanthro[10,1-b,c]-azepine (2), a homologue of apomorphine (1), has been found to be devoid of dopaminergic effects. The biological differences between apomorphine and this homologue are explained in terms of differences in conformation of the two molecules.     

Immunoassay for lysine8-vasopressin (LVP): Comparison of biological and immunological activity of lysine-vasopressin and some of its synthetic analogues

Résumé Ces résultats suggèrent d'une part que¹²⁵I-LVP monoiodée a peu d'activité antidiurétique, d'autre part que le noyau phénylalanine en position 3 est essentiel pour la liaison de l'antigène à l'anticorps et que les sites immunologiques et biologiques de l'hormone sont différents.

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Acknowledgments. We wish to thank ProfessorS. Jard (Collège de France, 11, place Marcellin Berthelot, Paris 5^eme) for his valuable advice in connection with this work. LVP analogues were generously supplied by Dr.R. A. Boissonnas of Sandoz Pharmaceuticals.     

Relationship between the structure of a series of carbamate derivatives of methomyl and their biological activity

Cellular and Molecular Life Sciences - A series of 24 carbamates was obtained by structural modification of methomyl, or S-methyl-N[(methylcarbamoyl)oxy]thioacetimidate, an insecticide. The...     

Relationship between the chemical structure of thiazolidine acetic acid derivatives and the antiherpetic activity in human embryonic cell cultures

Zusammenfassung Durch Abwandlung der Struktur der 4-Oxo-5-thiazolidinessigsäure ergeben sich starke inhibitorische Effekte auf die cytopathogenen Wirkungen, die vom VirusHerpes simplex in Kulturen menschlicher Embryonalzellen ausgeübt werden.     

MLL5 (KMT2E): structure,function, and clinical relevance

The mixed lineage leukemia (MLL) family of genes, also known as the lysine N-methyltransferase 2 (KMT2) family, are homologous to the evolutionarily conserved trithorax group that plays critical roles in the regulation of homeotic gene (HOX) expression and embryonic development. MLL5, assigned as KMT2E on the basis of its SET domain homology, was initially categorized under MLL (KMT2) family together with other six SET methyltransferase domain proteins (KMT2A–2D and 2F–2G). However, emerging evidence suggests that MLL5 is distinct from the other MLL (KMT2) family members, and the protein it encodes appears to lack intrinsic histone methyltransferase (HMT) activity towards histone substrates. MLL5 has been reported to play key roles in diverse biological processes, including cell cycle progression, genomic stability maintenance, adult hematopoiesis, and spermatogenesis. Recent studies of MLL5 variants and isoforms and putative MLL5 homologs in other species have enriched our understanding of the role of MLL5 in gene expression regulation, although the mechanism of action and physiological function of MLL5 remains poorly understood. In this review, we summarize recent research characterizing the structural features and biological roles of MLL5, and we highlight the potential implications of MLL5 dysfunction in human disease.     

Effects of [N-(2-oxo-3,5,7-cycloheptatrien-1-yl)] aminooxoacetic acid ethyl ester (AY-25,674) on cyclic 3′,5′-nucleotide formation and phosphodiesterase activity

Summary The orally-effective antiallergic compound [N-(2-oxo-3,5,7-cycloheptatrien-1-yl)] aminooxoacetic acid ethyl ester (AY-25,674) exhibited a potency equivalent to or 3 times less than theophylline in inhibiting guinea-pig lung and beef heart PDE, respectively. AY-25,674 did not affect the basal activity of guinea-pig lung adenyl cyclase. Although part of the antiallergic activity of AY-25,674 may be due to the ability to elevate cyclic AMP levels by PDE inhibition, other modes of action appear to be of greater relevance.The authors acknowledge the excellent technical assistance of Ms M.T. Silvestre.     

Effects of [N-(2-oxo-3,5,7-cycloheptatrien-1-yl)] aminooxoacetic acid ethyl ester (AY-25,674) on cyclic 3',5'-nucleotide formation and phosphodiesterase activity.

The orally-effective antiallergic compound [N-(2-oxo-3,5,7-cycloheptatrien-1-yl)] aminooxoacetic acid ethyl ester (AY-25,674) exhibited a potency equivalent to or 3 times less than theophylline in inhibiting guinea-pig lung and beef heart PDE, respectively, AY-25,674 did not affect the basal activity of guinea-pig lung adenyl cyclase. Although part of the antiallergic activity of AY-25,674 may be due to the ability to elevate cyclic AMP levels by PDE inhibition, other modes of action appear to be of greater relevance.     

The molecular structure of the benzilic acid rearrangement product of 3α, 17β-diacetoxy-11-hydroxy-12-oxo-5β-androst-9(11)-ene

Zusammenfassung Die Struktur desp-Brombenzoates des Benzilsäureumlagerungsproduktes von 3, 17-Diacetoxy-11-hydroxy-12-oxo-5-9(11)-androsten wurde durch dreidimensionale Röntgenstrukturanalyse eines Einkristalls als 3-p-Brombenzoat des 11-Carboxy-3, 11, 17-trihydroxy-13-C-nor-5-androstan 11a, 17-Laktons erkannt.     

Toxicity of benzenethiol and its derivatives onMusca domestica (DDT-resistant strain) and onPeriplaneta americana

Riassunto Gli autori hanno studiato la tossicità del tiofenolo a di alcuni suoi derivati per gli insetti. Il tiofenolo si è rivelato notevolmente tossico sia perPeriplaneta americana che perMusca domestica (ceppo resistente al DDT), mentre la maggior parte dei suoi derivati è fornita di scarsa tossicità.