Rhodium-catalyzed C-H carboxymethylation of anilines with vinylene carbonate.

A rhodium-catalyzed synthesis of phenylacetate has been realized by direct C-H carboxymethylation of anilines bearing removable directing groups. The reaction occurred most efficiently in air, without any external base or oxidant. This methodology is expected to provide a facile and general access to various bioactive 2-amino aromatic acetic acid derivatives.

Spatio-temporal distribution and overlap of and in Gongga Mountain, Sichuan, China.

Clarifying the distribution pattern and overlapping relationship of sympatric relative species in the spatio-temporal niche is important for our understanding of the behavioral relationship between species and the integrated management of multi-species habitats. Based on the infrared camera monitoring data from 2012 to 2021, we investigted the spatio-temporal distribution characteristics of the national secondary-class key protected animals and in the Gongga Mountain National Nature Reserve, Sichuan Province. We analyzed the distribution of and .

Recent advance of small-molecule drugs for clinical treatment of multiple myeloma.

Multiple myeloma (MM) is a hematologic neoplasm of plasma cells that is currently deemed incurable. Despite the introduction of novel immunomodulators and proteasome inhibitors, MM remains a challenging disease with high rates of relapse and refractoriness. The management of refractory and relapsed MM patients remains a formidable task, primarily due to the emergence of multiple drug resistance.

C-H acylation of aniline derivatives with α-oxocarboxylic acids using ruthenium catalyst.

An efficient and convenient synthetic strategy for ruthenium(II)-catalyzed -acylation of -(2-pyridyl)-anilines using α-oxycarboxylic acids as acyl sources is described. The procedure can smoothly proceed under mild conditions, showing good functional group tolerance. Valuable -acylated aniline products have been obtained with moderate to good yields.

Rhodium-Catalyzed Azine-Directed C-H Amidation with -Methoxyamides.

Using -methoxyamide reagents as an amide source, C-H amidation was realized at the ortho position of azine under the action of rhodium and boric acid. The method has mild reaction conditions, high atomic utilization, excellent yield, and wide adaptability to amidation reagents (both aromatic amides and fatty amides are applicable). Amide-substituted ketones can be obtained by a simple treatment and can be further transformed into bioactive substances.

Rhodium-Catalyzed C(sp)-H Amidation of Azine with Sulfonamides.

Direct C-H amidation of azine with sulfonamide was developed for the first time. The reactions proceeded smoothly under benign conditions and gave the corresponding products with high selectivity. This approach shows high regioselectivity, wide substrate scope, and functional group tolerance.

[Application of relative quality constant in grades evaluation of bran stir-baked Aurantii Fructus].

The specifications of Chinese herbal medicines naturally form and exist in the circulation and use of Chinese herbal medicines.Buyers and sellers negotiate price by quality. With the increasing demand for public health care,the cultivation,processing methods and circulation of Chinese herbal medicines have changed.

Risk factors for postoperative stroke in adults patients with moyamoya disease: a systematic review with meta-analysis.

Background: This systematic review and meta-analysis aimed to clarify the risk factors for postoperative stroke in adult patients with moyamoya disease (MMD).

Methods: We comprehensively searched MEDLINE/PubMed, Web of Science, and Cochrane Library for eligible published literature with regard to the risk factors and postoperative complications in adult patients with MMD. Statistical analysis was conducted using Stata version 12.

An anatomic study of trifurcate iliotibial bands for correcting valgus knee deformity.

Background: The iliotibial band (ITB) trifurcates into the anterior, central and posterior branches at the knee level, and sometimes the branches must be selectively released to correct the valgus knee deformity during total knee arthroplasty. However, the anatomical morphology of the trifurcate ITBs has not been investigated.

Methods: Fifty-two knees from 26 embalmed cadavers were dissected to observe and record the relationship of the three branches given off from the ITB trifurcation.

A facile three-step total synthesis of tanshinone I.

A facile synthetic approach for total synthesis of tanshinone I has been accomplished. The key precursor is a novel compound, epoxy phenanthraquinone. And this synthesis of tanshinone I is achieved in only three simple stages, which include Diels-Alder reaction, Δ(2)-Weitz-Scheffer-type epoxidation, and Feist-Bénary reaction from commercially available styrene.

Reversal of P-gp and BCRP-mediated MDR by tariquidar derivatives.

With an aim to generate non-toxic, specific and highly potent multidrug resistance (MDR) modulators, a novel series of anthranilic acid amide-substituted tariquidar derivatives were synthesized. The new compounds were evaluated for their cytotoxicity toward normal human colon fibroblasts (CCD18-Co), human gastric epithelial cell line (HFE) and primary rat liver cells, and for their ability to inhibit P-gp/BCRP-mediated drug efflux and reversal of P-gp and BCRP-mediated MDR in parental and drug-resistant cancer cell lines (LCC6 MDR1, MCF-7 FLV1000, R-HepG2, SW620-Ad300). While tariquidar is highly toxic to normal cells, the new derivatives exhibited much lower or negligible cytotoxicity.

Evaluation and SAR analysis of the cytotoxicity of tanshinones in colon cancer cells.

Aim: This study was designed to evaluate the anti-cancer actions of tanshinone I and tanshinone IIA, and six derivatives of tanshinone IIA on normal and cancerous colon cells. Structure activity relationship (SAR) analysis was conducted to delineate the significance of the structural modifications of tanshinones for improved anti-cancer action.

Method: Tanshinone derivatives were designed and synthesized according to the literature.

Eremophilenolides and other constituents from the roots of Ligularia sagitta.

Chemical investigation of the roots of Ligularia sagitta has resulted in the characterization of six eremophilenolides 6beta,8beta-dimethoxy-10beta-hydroxyeremophil-7(11)-en-12,8alpha-olide (1), 6beta-angeloyloxy-10beta-hydroxy-8beta-methoxyeremophil-7(11)-en-12,8alpha-olide (2), 6beta-(2'-methylbutanoyloxy)-10beta-hydroxy-8beta-methoxyeremophil-7(11)-en-12,8alpha-olide (3), 6beta-angeloyloxy-10beta-hydroxy-8alpha-methoxyeremophil-7(11)-en-12,8beta-olide (4), 6beta-(2'-methylbutanoyloxy)-10beta-hydroxy-8alpha-methoxyeremophil-7(11)-en-12,8beta-olide (5) and 8beta,10beta-dihydroxy-6beta-methoxyeremophil-7(11)-en-12,8alpha-olide (6), together with one monoterpene (3 R,4 R,6 S)-3,6-dihydroxy-1-menthene (7), two triterpenes lupeol (8) and ursolic acid (9), and beta-sitosterol (10). The structures of five new constituents (1-5) were elucidated by spectroscopic methods including 2D-NMR experiments. The compounds 1, 5 and 7 showed antibacterial activity by being assayed against Staphylococcus aureus, Bacillus subtilis and Escherichia coli.