Head-to-head bisbenzazole derivatives as antiproliferative agents: design,synthesis, in vitro activity,and SAR analysis

Molecular Diversity - In the present work, a series of bisbenzazole derivatives were designed and synthesized as antiproliferative agents. The antiproliferative activity of these compounds was...     

Thermally stimulated current measurements in as-grown TlGaSeS layered single crystals

Charge carrier traps in as-grown TlGaSeS layered single crystals were studied using thermally stimulated current measurements. The investigations were performed in temperatures ranging from 10 to 100 K. The experimental evidences were found for the presence of one shallow hole trapping center in TlGaSeS, located at 12 meV from the valence band. The trap parameters have been calculated using various methods of analysis, and these agree well with each other. Its capture cross-section and concentration have been found to be 8.9 × 10⁻²⁶ cm² and 2.0 × 10¹⁴ cm⁻³, respectively. Analysis of the thermally stimulated current data at different light excitation temperatures leads to a value of 19 meV/decade for the shallow hole traps distribution.     

The mid-level hump at 2 kHz

Shortening the duration of a Gaussian-shaped 2-kHz tone-pip causes the intensity-difference limen (DL) to depart from the "near-miss to Weber's law" and swell into a mid-level hump [Nizami et al., J. Acoust. Soc. Am. 110, 2505-2515 (2001)]. For some subjects the size of this hump approaches or exceeds the size reported for longer tones under forward masking, suggesting that forward masking might make little difference to the DL for very brief probes. To test this hypothesis, DLs were determined over 30 to 90 dB SPL for a brief Gaussian-shaped 2-kHz tone-pip. DLs were obtained first without forward masking, then with the pip placed 10 or 100 ms after a 200-ms 2-kHz tone of 50 dB SPL, or 100 ms after a 200-ms 2-kHz tone of 70 dB SPL. DLs inflated significantly under all forward-masking conditions. DLs also enlarged under an 80 dB SPL forward masker at pip delays of 4, 10, 40, and 100 ms. The peaks of the humps obtained under forward masking clustered around a sensation level (SL) that was significantly lower than the average SL for the peaks of the humps obtained without forward masking. Overall, the results do not support the neuronal-recovery-rate model of Zeng et al. [Hear. Res. 55, 223-230 (1991)], but are not incompatible with the Carlyon and Beveridge hypothesis [J. Acoust. Soc. Am. 93, 2886-2895 (1993)] that nonsimultaneous maskers corrupt the memory trace evoked by the probe.     

Synthesis of 3H-naphtho[2.1-b]pyran-2-carboxamides from cyclocoupling of β-naphthol,propargyl alcohols and isocyanide in the presence of Lewis acids

3H-Naphtho[2.1-b]pyran-2-carboxamides (3H-Benzo[f]chromene-2-carboxamides) can be synthesized from a three-component cyclocoupling reaction of β-naphthol, propargyl alcohols and isocyanide in the presence of ZnI₂ and FeCl₃ under air atmosphere. The reaction is proposed to involve the formation of aryl-zinc (II) σ-bond and its α-addition to isocyanide.     

Structural determination of salsolins A and B, new antioxidant polyoxygenated triterpenes from Salsola baryosma, by 1D and 2D NMR spectroscopy

Salsolins A (1) and B (2), the new triterpenes, have been isolated from the chloroform soluble fraction of Salsola baryosma along with 2alpha,3beta,23,24-tetrahydroxyurs-12-en-28-oic acid (3) reported for the first time from this species. Their structures have been assigned from 1H and 13C NMR spectra, DEPT and by 2D COSY, NOESY, HMQC and HMBC experiments. The compounds 1-3 showed significant antioxidant activity.     

Determination of deep trapping center parameters in as-grown Tl2Ga2S3Se layered crystals

Thermally stimulated current measurements were carried out on as-grown Tl₂Ga₂S₃Se layered single crystals. The investigations were performed in temperatures ranging from 10 to 320 K with heating rates of 0.6–1.2 K s⁻¹. The analysis of the data revealed the hole trap level located at 498 meV. The activation energies of the traps have been determined using various methods of analysis, and they agree with each other. The calculation for these traps yielded 2.1 × 10⁻¹⁸ cm² for capture cross-section and 2.3 × 10⁹ cm⁻³ for the concentration. It was concluded that in this center retrapping was negligible, as confirmed by the good agreement between the experimental results and the theoretical predictions of the model that assumes slow retrapping.     

On differential equations with interval coefficients

In this study, a new approach is developed to solve the initial value problem for interval linear differential equations. In the considered problem, the coefficients and the initial values are constant intervals. In the developed approach, there is no need to define a derivative for interval-valued functions. All derivatives used in the approach are classical derivatives of real functions. The reason for this is that the solution of the problem is defined as a bunch of real functions. Such a solution concept is compatible also with the robust stability concept. Sufficient conditions are provided for the solution to be expressed analytically. In addition, on a numerical example, the solution obtained by the proposed approach is compared with the solution obtained by the generalized Hukuhara differentiability. It is shown that the proposed approach gives a new type of solution. The main advantage of the proposed approach is that the solution to the considered interval initial value problem exists and is unique, as in the real case.     

A Genetic Algorithm for the Set Covering Problem

In this paper, the set covering problem (SCP) is considered. Several algorithms have been suggested in the literature for solving it. We propose a new algorithm for solving the SCP which is based on the genetic technique. This algorithm has been implemented and tested on various standard and randomly generated test problems. Preliminary results are encouraging, and are better than the existing heuristics for the problem.     

2‐(2,1‐Benzoxazol‐3‐yl)‐3,5‐di­methoxy­phenol and 3‐phenyl‐2,1‐benzoxazole

The title compounds, C₁₅H₁₃NO₄, (I), and C₁₃H₉NO, (II), are produced, along with the corresponding anilines, by the reduction of the appropriate o‐nitro­benzo­phenones. In (I), the planar benz­isoxazole and phenol fragments are tilted relative to one another by a rotation of 53.02 (14)° about the bond joining them, and the mol­ecules are linked into chains by phenol O—H...N and phenyl C—H...O_oxazole hydrogen bonds. The cell of (II) (space group I2/c) contains eight mol­ecules in general positions, four more in the 2b sites, with twofold axial symmetry that induces a degree of disorder, and a further four as centrosymmetric pairs of complete mol­ecules, each with an occupancy of one‐half. The relative tilt of the planar fragments varies slightly from one mol­ecule to another but is much less than that in (I), ranging from 8.8 (8) to 12.58 (15)°.