Design, synthesis and anti-tumor efficacy evaluation of novel 1,3-diaryl propane-based polyphenols obtained from Claisen rearrangement reaction.

Polyphenols such as resveratrol, honokiol and nordihydroguaiaretic acid are widely existing in nature products or synthetic compounds with interesting biological activities. Inspired by their structural feature, a total of 49 1,3-diaryl propane-based polyphenols were designed and synthesized through Claisen rearrangement reaction. New compounds were initially assessed for their anti-proliferative activities against various cancer cell lines (PC-3, U87MG, U251, HCT116) at a concentration of 50 μM, and the results guided the SAR of this series of compounds.

Design, synthesis and antitumor efficacy evaluation of a series of novel β-elemene-based macrocycles.

β-Elemene is the major constituent of the antitumor drugs elemene extract approved in China. By incorporating macrocyclization strategy into the β-elemene skeleton, we designed a series of novel macrocycles retaining three key carbon-carbon double bonds. Four different methods have been successfully developed for these challenging ring systems.

Recent Progress in Fragmentation of Katritzky Salts Enabling Formation of C-C, C-B, and C-S Bonds.

Since their discovery in 1970s, Katritzky salts have emerged as one of the most important classes of building blocks for use in organic synthesis and drug discovery. These bulky pyridinium salts derived from alkylamine can readily generate alkyl radical and undergo a variety of organic transformation reactions such as alkylation, arylation, alkenylation, alkynylation, carbonylation, sulfonylation, and borylation. Through these transformations, complexed molecules bearing new C-C, C-B, or C-S bonds can be constructed in easy ways and in simple steps.

Recent Advances in Synergistic Antitumor Effects Exploited from the Inhibition of Ataxia Telangiectasia and RAD3-Related Protein Kinase (ATR).

As one of the key phosphatidylinositol 3-kinase-related kinases (PIKKs) family members, ataxia telangiectasia and RAD3-related protein kinase (ATR) is crucial in maintaining mammalian cell genomic integrity in DNA damage response (DDR) and repair pathways. Dysregulation of ATR has been found across different cancer types. In recent years, the inhibition of ATR has been proven to be effective in cancer therapy in preclinical and clinical studies.

Races of small molecule clinical trials for the treatment of COVID-19: An up-to-date comprehensive review.

The coronavirus disease-19 (COVID-19) pandemic has become a global threat since its first outbreak at the end of 2019. Several review articles have been published recently, focusing on the aspects of target biology, drug repurposing, and mechanisms of action (MOAs) for potential treatment. This review gathers all small molecules currently in active clinical trials, categorizes them into six sub-classes, and summarizes their clinical progress.

Nickel-catalyzed enantioselective 1,2-vinylboration of styrenes.

A novel nickel-catalyzed asymmetric 1,2-vinylboration reaction has been developed to afford benzylic alkenylboration products with high yields and excellent enantioselectivities by using a chiral bisoxazoline ligand. Under optimized conditions, a wide variety of chiral 2-boryl-1,1-arylvinylalkanes are efficiently prepared from readily available olefins and vinyl halides in the presence of bis(pinacolato)diboron as the boron source in a mild and easy-to-operate manner. This three-component cascade protocol furnishes exceptional chemo- and stereoselectivity, and its usefulness is illustrated by its application in asymmetric modifications of several structurally complex natural products and pharmaceuticals.

Establishment of predictive model for analyzing clinical pregnancy outcome based on IVF-ET and ICSI assisted reproductive technology.

Unlabelled: In order to explore the predictive model for analyzing clinical pregnancy outcomes based on IVF-ET (in vitro fertilization and embryo transfer) and ICSI (Intracytoplasmic sperm injection) assisted reproductive technology (ART).

Methods: this study selected the embryo transfer (fresh) patients who received IVF-ET or ICSI treatment in the First Affiliated Hospital of Guangxi Medical University as the subjects. Moreover, the controlled ovarian stimulation (COS) and follow-up were conducted to collect relevant data for analysis, and finally a prediction model was established.