Synthesis and bioactivity evaluation of pachymic acid derivatives as potential cytotoxic agents [0.03%]
作为潜在细胞毒性剂的千层纸酸衍生物的合成及其生物活性评价
Hezhen Wang,Xun Sun,Chunyong Wei et al.
Hezhen Wang et al.
Pachymic acid, a well-known natural lanostane-type triterpenoid, exhibits various pharmacological properties. In this study, 18 derivatives of pachymic acid were synthesized by modifying their molecular structures and evaluated for their an...
Synthesis of 2-Oxoquinoline Derivatives as Dual Pim and mTORC Protein Kinase Inhibitors [0.03%]
作为双重Pim和mTORC蛋白激酶抑制剂的2-氧代喹啉衍生物的合成
Giri R Gnawali,Koichi Okumura,Karolina Perez et al.
Giri R Gnawali et al.
Compound VBT-5445 was identified as an inhibitor to block the association of Pim and the protein Enhancer of Decapping 3 (EDC3), a Pim substrate, which normally functions to enhance the decapping of messenger RNA (mRNA). It was also shown t...
RNA-dependent RNA polymerase (RdRp) natural antiviral inhibitors: a review [0.03%]
基于RNA的RNA聚合酶(RdRp)天然抗病毒抑制剂的研究进展综述
Daniela Regina Buch Leite,Karen Mary Mantovani,Solange Pereira Cordeiro et al.
Daniela Regina Buch Leite et al.
Viral diseases are the cause of many global epidemics, leading to deaths, affecting the quality of life of populations, and impairing public health. The limitations in the treatment of viral diseases and the constant resistance to conventio...
Synthesis and biological evaluation of (+)-paeoveitol derivatives as novel antidepressants [0.03%]
新型抗抑郁剂（+）-MPEVE衍生物的合成与生物学评价
Tian-Ze Li,Xiao-Yan Huang,Jin-Jin Sun et al.
Tian-Ze Li et al.
The antidepressant activity of (+) and (-)-paeoveitol was first evaluated using the forced swimming test (FST), and (+)-paeoveitol showed potential antidepressant activity by decreasing immobility time of mice (by approximately 26.4%) in th...
Discovery of mobocertinib, a new irreversible tyrosine kinase inhibitor indicated for the treatment of non-small-cell lung cancer harboring EGFR exon 20 insertion mutations [0.03%]
莫博赛替尼：首个针对非小细胞肺癌EGFR 20号外显子插入突变的不可逆酪氨酸激酶抑制剂的研发历程
Jun Wang,Daniel Lam,Jeffrey Yang et al.
Jun Wang et al.
Epidermal growth factor receptor (EGFR) is essential for normal cellular functions. Mutations of EGFR's kinase domain can cause dysregulation leading to non-small cell lung cancer (NSCLC). Exon 20 insertion (ex20ins) mutations in EGFR are o...
The history, mechanism, and perspectives of nirmatrelvir (PF-07321332): an orally bioavailable main protease inhibitor used in combination with ritonavir to reduce COVID-19-related hospitalizations [0.03%]
尼马特瑞韦(PF-07321332)的前世、今生和未来：与利托那韦联用减少新冠住院率的口服主蛋白酶抑制剂
Ryan P Joyce,Vivian W Hu,Jun Wang
Ryan P Joyce
The rapid development of effective vaccines to combat the SARS-CoV-2 virus has been an effective counter measure to decrease hospitalization and the mortality rate in many countries. However, with the risk of mutated strains decreasing the ...
Merging antimicrobial and visible emission properties within 1,3,4-trisubstituted-1,2,3-triazolium salts [0.03%]
兼具抗菌和可见发射性能的1,3,4-三取代-1,2,3-三氮唑
Connor A Lejcher,Eric M Villa,James T Fletcher
Connor A Lejcher
Bioactive molecules displaying visible wavelength emission can be useful for bioimaging, chemosensing and photodynamic therapy applications. Reported herein are 1,3,4-trisubsituted-1,2,3-triazolium salts displaying both antimicrobial and vi...
Design and synthesis of ludartin derivatives as potential anticancer agents against hepatocellular carcinoma [0.03%]
作为抗肝细胞癌剂的卢达汀衍生物的设计与合成
Jin-Jin Sun,Jin-Ping Wang,Tian-Ze Li et al.
Jin-Jin Sun et al.
Our previous study demonstrated that guaiane-type sesquiterpenoid ludartin showed potent antihepatoma activity against two human hepatocellular carcinoma cell lines, HepG2 and Huh7, with IC50 values of 32.7 and 34.3 μM, respectively. In th...
Design, synthesis and evaluation of amino-3,5-dicyanopyridines and thieno[2,3-b]pyridines as ligands of adenosine A1 receptors for the potential treatment of epilepsy [0.03%]
作为腺苷A1受体配体的氨基-3,5-二氰基吡啶和噻诺并[2,3-b]吡啶的设计、合成与评价（用于治疗癫痫）
Gaofenngwe Nkomba,Gisella Terre&#x;Blanche,Helena D Janse van Rensburg et al.
Gaofenngwe Nkomba et al.
Due to the implication of adenosine in seizure suppression, adenosine-based therapies such as adenosine receptor (AR) agonists have been investigated. This study aimed at investigating thieno[2,3-b]pyridine derivatives as non-nucleoside A1 ...
Invalidation of dieckol and 1,2,3,4,6-pentagalloylglucose (PGG) as SARS-CoV-2 main protease inhibitors and the discovery of PGG as a papain-like protease inhibitor [0.03%]
黛克醇和1,2,3,4,6-五没食子酰葡萄糖(PGG)不是SARS-CoV-2主要蛋白酶抑制剂及PGG是裂解酶样半胱氨酸蛋白酶抑制剂的发现
Haozhou Tan,Chunlong Ma,Jun Wang
Haozhou Tan
The COVID-19 pandemic spurred a broad interest in antiviral drug discovery. The SARS-CoV-2 main protease (Mpro) and papain-like protease (PLpro) are attractive antiviral drug targets given their vital roles in viral replication and modulati...