Modular Synthetic Approach to Carboranyl‒Biomolecules Conjugates

The development of novel, tumor-selective and boron-rich compounds as potential agents for use in boron neutron capture therapy (BNCT) represents a very important field in cancer treatment by radiation therapy. Here, we report the design and synthesis of two promising compounds that combine meta-carborane, a water-soluble monosaccharide and a linking unit, namely glycine or ethylenediamine, for facile coupling with various tumor-selective biomolecules bearing a free amino or carboxylic acid group. In this work, coupling experiments with two selected biomolecules, a coumarin derivative and folic acid, were included. The task of every component in this approach was carefully chosen: the carborane moiety supplies ten boron atoms, which is a tenfold increase in boron content compared to the l-boronophenylalanine (l-BPA) presently used in BNCT; the sugar moiety compensates for the hydrophobic character of the carborane; the linking unit, depending on the chosen biomolecule, acts as the connection between the tumor-selective component and the boron-rich moiety; and the respective tumor-selective biomolecule provides the necessary selectivity. This approach makes it possible to develop a modular and feasible strategy for the synthesis of readily obtainable boron-rich agents with optimized properties for potential applications in BNCT.     

Synthesis and characterization of modular polyphosphonate homopolymers and copolymers

Linear polyphosphonates with the generic formula –[P(Ph)(X)OR′O]_n– (X = S or Se) have been synthesized by polycondensations of P(Ph)(NEt₂)₂ and a diol (HOR′OH = 1,4-cyclohexanedimethanol, 1,4-benzenedimethanol, tetraethylene glycol, or 1,12-dodecanediol) followed by reaction with a chalcogen. Random copolymers have been synthesized by polycondensations of P(Ph)(NEt₂)₂ and mixture of two of the diols in a 2:1:1 mol ratio followed by reaction with a chalcogen. Block copolymers with the generic formula –[P(Ph)(X)OR′O]_{(x + 2)} –[P(Ph)(X)OR′O]_{(x + 3)}– (X = S or Se) have been synthesized by the polycondensations of Et₂N[P(Ph)(X)OR′O]_{(x + 2)}P(Ph)NEt₂ oligomers with HOR′O[P(Ph)(X)OR′O]_{(x + 3)}H oligomers followed by reaction with a chalcogen. The Et₂N[P(Ph)(X)OR′O]_{(x + 2)}P(Ph)NEt₂ oligomers are prepared by the reaction of an excess of P(Ph)(NEt₂)₂ with a diol while the HOR′O[P(Ph)(X)OR′O]_{(x + 3)}H oligomers are prepared by the reaction of P(Ph)(NEt₂)₂ with an excess of the diol. In each case the excess, x is the same and determines the average block sizes. All of the polymers were characterized using ¹H, ¹³C{¹H}, and ³¹P{¹H} NMR spectroscopy, TGA, DSC, and SEC. ³¹P{¹H} NMR spectroscopy demonstrates that the random and block copolymers have the expected arrangements of monomers and, in the case of block copolymers, verifies the block sizes. All polymers are thermally stable up to ~300°C, and the arrangements of monomers in the copolymers (block vs. random) affect their degradation temperatures and T_g profiles. The polymers have weight average MWs of up to 3.8 × 10⁴ Da.     

Koszul filtrations and finite lattices

In this note, we characterize when a finite lattice is distributive in terms of the existences of some particular classes of Koszul filtrations.     

Modular Synthesis of Triarylamines and Poly(triarylamine)s through a Radical Mechanism

A modular protocol for the triarylamine synthesis has been developed using diarylamines and electron-rich arenes, such as phenols, as the building blocks. The KI/KIO₄ system proves to be highly efficient for the cross-dehydrogenative coupling of phenothiazines/phenoxazines with phenols/anilines. A wide range of functional groups attached to both coupling partners were well tolerated. Through the manipulation of reaction temperatures, the sequential assembly of bis-triarylamines could be achieved to provide the unsymmetrically bis-aminated phenols efficiently. Furthermore, the multiple aminated polyphenols were rapidly constructed in good to high yields by a single operation.     

多重调和Bergman空间上径向Toeplitz算子的交换性

In this paper, we study the commutativity of Toeplitz operators with radial symbols on the pluriharmonic Bergman space. We obtain the necessary and sufficient conditions for the commutativity of bounded Toeplitz operator and Toeplitz operator with radial symbol on the pluriharmonic Bergman space.     

基于能力培养的应用型本科物理实验教学模式探索

通过对传统大学物理实验教学现状的分析和讨论,针对目前大学物理实验课程的教学模式进行研究,在遵循实验教学自身规律的前提下,构建“模块化”实验课程教学模式,从而改善课程结构,为培养学生解决具体问题的实践能力和创新思维提供针对性的训练;并采用“启发式”“问题式”的教学方法和多样化的考核评价标准,对于不同专业、不同基础、不同背景的学生进行差异化教学,建立以人才培养为核心的科学教学体系,进一步提高大学物理实验课程的教学质量和效果.     

Modular class primes in the Sundaram sieve

The purpose of this paper is to consider analogues of the twin-prime conjecture in various classes within modular rings.