Structure-activity relationship studies were conducted on Irosustat (STX64, BN83495), the first steroid sulfatase (STS) inhibitor to enter diverse clinical trials for patients with advanced hormone-dependent cancer. The size of its aliphatic ring was expanded; its sulfamate group was N,N-dimethylated, relocated to another position and flanked by an adjacent methoxy group; and series of quinolin...

Two ergostanes, 5α,8α-epidioxy-22E-ergosta-6,22-dien-3β-ol (1) and 5α-ergost-7,22-dien-3β-ol (2), and a lanostane, 3β-hydroxylanostan-8,24-diene-21-oic acid (trametenolic acid) (3), were isolated from an n-hexane extract prepared from the fruiting body of Trametes versicolor (Bres. Rivarden). The activity of the isolated sterols was evaluated against promastigotes and amastigotes of Leishmania ...

The purpose of this study was to characterize the kinetics and voltage-dependence of the block of N-methyl-D-aspartate (NMDA)-induced currents in primary cultures of rat cortical neurons by the neuroprotective, low-affinity, NMDA antagonist ARL 15896AR, using whole-cell voltage-clamp techniques. ARL 15896AR caused rapid and reversible inhibition of NMDA (50 microM)-evoked currents from neurons ...

completely novel structure in this class of compounds. Fermentation and Isolation Cremeomycinwas originally reported by Bergy and Pyke at the Upjohn Company in 1967 from Streptomyces cremeus NRRL3241.11} Neither a structural formula nor functional group information was reported. Physico-chemical and Biological Properties Cremeomycinis a bright yellow solid that is soluble in solvents from dichl...

Abstract. Low-energy dipole excitations have been investigated theoretically in N=50 Sr and Zr, several N=82 isotones and the Z = 50 Sn isotopes. For this purpose a method incorporating both HFB and multi-phonon QPM theory is applied. A concentration of one-phonon dipole strength located below the neutron emission threshold has been calculated in these nuclei. The analysis of the corresponding ...

Article history: Received on: 09/07/2013 Revised on: 29/07/2013 Accepted on: 14/09/2013 Available online: 30/09/2013 Extracts and fractions from the leaves and stems of Tetracera breyniana Schltdl. were evaluated against the fourth instar Aedes aegypti larvae and ability to scavenge free radicals. Fractions that provided the best results were fractionated on silica gel column to afforded three ...

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Ottonia martiana is a plant popularly known in Brazil by the use for toothache. Ethanolic extract (EE), hexane fraction (HF), dichloromethane fraction (DF) and piperovatine obtained from O. martiana were assayed in vitro and in vivo. The acute toxicity of EE was determined, and LD50 values of 164.5 and 65.0 mg/kg by the oral and intraperitoneal routes, respectively, indicated a high toxicity fo...