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Renal cell carcinoma escapes death by p53 depletion through transglutaminase 2-chaperoned autophagy
Along with the increase in p53 stability due to TGase 2 inhibition, the administration of a DNA-damaging anti-cancer drug such as doxorubicin-induced apoptosis in RCC cell lines and synergistically reduced tumor volume in a xenograft model may represent an effective therapeutic approach for treating RCC.
Regioselective synthesis of 2-amino-substituted 1,3,4-oxadiazole and 1,3,4-thiadiazole derivatives via reagent-based cyclization of thiosemicarbazide intermediate.
- S. Yang, Seokju Lee, Hyun-Jung Kwak, Y. Gong
- ChemistryThe Journal of organic chemistry
- 18 January 2013
A regioselective, reagent-based method for the cyclization reaction of 2-amino-1,3,4-oxadiazole and 2-amino-1,3,4-thiadiazole core skeletons is described. The thiosemicarbazide intermediate 3 was…
A Highly Efficient Diversification of 2-Amino/Amido-1,3,4-oxadiazole and 1,3,4-Thiadiazole Derivatives via Reagent-Based Cyclization of Thiosemicarbazide Intermediate on Solid-Phase.
The constructed library shows reasonable, oral bioavailability drug properties as determine by using the Lipinski's Rule and similar parameters.
A Novel Solid-Phase Synthetic Method for 1,4-Benzodiazepine-2,5-dione Derivatives
Using polymer-bound anthranilic acid derivatives, the 1,4-benzodiazepine-2,5-dione derivatives 3 were obtained through an unprecedented reaction sequence, reductive alkylation-N-protected amino acid coupling-deprotective cyclization, in 28-71% five-step overall isolated yields and 95-99% purities from Wang resin 4.
A novel sphingosylphosphorylcholine and sphingosine-1-phosphate receptor 1 antagonist, KRO-105714, for alleviating atopic dermatitis
The data suggest that SPC and S1P1 antagonist KRO-105714 has the potential to alleviate atopic dermatitis.
Unexpected Route for the Synthesis of N,N‐Dialkyl Formamidines Using Phenyl Chloroformate and N,N‐Dialkyl Formamides.
It is discovered that phenyl chloroformate can be used as an efficient dehydrating agent for the synthesis of formamides from a variety of primary amines and N,N-dialkyl formamides by using short…
Novel Inhibitors of Prolyl 4-Hydroxylase; Solid-phase Synthesis of 2,2-Dimethyl-3,4-Dialkoxy-Substituted 6-Aminobenzopyran Derivatives
2,2-Dimethyl-3,4-dialkoxy-substituted 6-aminobenzopyran analogues (eg., 7 and 8) were identified as prolyl 4-hydroxylase inhibitors via a screening process using HSC-T6 and LI 90 cells that express…
Microwave-Assisted Facile One-Step Carbamoylation of 6-Aminouracils
Carbamoylation of 6-aminouracils was achieved by reacting 6-aminouracils with isocyanates under computer-controlled microwave irradiation for a short reaction time. Under known thermal conditions,…
Synthesis, hypoglycemic and hypolipidemic activities of novel thiazolidinedione derivatives containing thiazole/triazole/oxadiazole ring.
Regioselective synthesis of dipyrrolopyrazine (DPP) derivatives via metal free and metal catalyzed amination and investigation of their optical and thermal properties
Pyrazine is an important molecular scaffold employed in organic optoelectronic materials. Here we report efficient methods for the synthesis of dipyrrolopyrazine, and pyrrolothieno-pyrazine…