Rhodium(III)-Catalyzed Regioselective C(sp)-H Functionalization of 7-Arylpyrazolo[1,5-]pyrimidines with Dioxazolones as Amidating Agents.

Rh(III)-catalyzed C-H functionalization of 7-arylpyrazolo[1,5-]pyrimidines was developed wherein the pyrazolo[1,5-]pyrimidine moiety is reported for the first time to direct the C-H bond activation. Various 7-arylpyrazolo[1,5-]pyrimidines underwent smooth C-H amidation with alkyl-, aryl-, and heteroaryl-substituted dioxazolones to afford the products in moderate to good yields. Mechanistic studies suggest that a six-membered rhodacycle intermediate involving N1 might play a key role in the regioselective catalytic cycle.

Review of Herbal Traditional Chinese Medicine for the Treatment of Diabetic Nephropathy.

Diabetic nephropathy (DN) is the most serious chronic complications of diabetes; 20-40% of diabetic patients develop into end stage renal disease (ESRD). However, exact pathogenesis of DN is not fully clear and we have great difficulties in curing DN; poor treatment of DN led to high chances of mortality worldwide. A lot of western medicines such as ACEI and ARB have been demonstrated to protect renal function of DN but are not enough to delay or retard the progression of DN; therefore, exploring exact and feasible drug is current research hotspot in medicine.

Hepatitis C virus-related heat-insoluble cryoglobulinemia and thrombotic microangiopathy.

Heat-insoluble cryoglobulinemia is rare, and its pathogenesis and comorbidities remain poorly understood. Here, the authors report a case of hepatitis C virus (HCV)-related heat-insoluble cryoglobulinemia associated with thrombotic microangiopathy and cryoglobulin-occlusive membranoproliferative glomerulonephritis. The patient, a 57-year-old woman, presented with acute kidney injury, thrombocytopenia, anemia with schistocytes, high levels of serum HCV RNA of HCV genotype 2a, rheumatoid factor positivity and high levels of serum immunoglobulin (Ig) M and Igκ.

A facile chemoenzymatic approach: one-step syntheses of monoterpenoid indole alkaloids.

Facile chemoenzymatic syntheses of cytotoxic monoterpenoid indole alkaloids with novel skeletons and multiple chiral centers are described. Synthesis of these alkaloids was achieved by a simple one-step reaction using strictosidine and 12-aza-strictosidine as the key intermediates. Strictosidines were prepared by coupling of secologanin with tryptamine and 7-aza-tryptamine, respectively, using the immobilized recombinant Rauvolfia strictosidine synthase.

Synthesis and structure-activity relationship studies of cytotoxic cinnamic alcohol derivatives.

Three series of di- and trisubstituted derivatives of cinnamic alcohol and its conjugated dienol analogues were designed and synthesised. The derivatives were screened for cytotoxicity against nine tumour cell lines: KB, A549, Hela, CNE, PC-3, BEL-7404, HL-60, BGC823 and P388D1. Most of the cinnamic alcohol derivatives showed cytotoxic activity.

Total synthesis and cytotoxicity evaluation of syrinenin-4-O-farnesylether and its analogues.

First synthesis of natural product, syrinenin-4-O-farnesylether (1), was carried out via two different paths. Four of its derivatives (9-12) were also prepared. Cytotoxicity screening of the selected compounds were performed on six tumour cell lines.

Design, synthesis, and SAR analysis of cytotoxic sinapyl alcohol derivatives.

Five series totalling 51 of sinapyl alcohol derivatives were designed and synthesized. Their cytotoxicity analyses were performed on six human tumor cell lines such as PC-3, CNE, KB, A549, BEL-7404, and HeLa. Certain sinapyl alcohol derivatives showed significant cytotoxic activities.

Synthesis and biological evaluation of a natural ester sintenin and its synthetic analogues.

Synthesis of 3-(3,4-dimethoxyphenyl)propyl-3-(3,4-dimethoxyphenyl) propanoate (18), a cytotoxic natural ester, was carried out by a convenient synthetic path with a total yield of 49%. Sixteen of its analogues (19-34) were also prepared. Seventeen unsaturated derivatives of 18, compounds 1-17, were also synthesized to examine the structure-activity relationship of this type of ester.