Journal of Medicinal Chemistry
Papers 10,000
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#1Federica GiordaniH-Index: 10
#2Abedawn I. KhalafH-Index: 14
view all 8 authors...
#1Xiao-Fei Chen (CAS: Chinese Academy of Sciences)H-Index: 1
#2Xin Zhao (CAS: Chinese Academy of Sciences)H-Index: 38
Last. Zifeng Yang (GMU: Guangzhou Medical University)H-Index: 23
view all 3 authors...
Nucleic acid aptamers are single-stranded DNA or RNA molecules selected in vitro that can bind to a broad range of targets with high affinity and specificity. As promising alternatives to conventional anti-infective agents, aptamers have gradually revealed their potential in the combat against infectious diseases. This article provides an overview on the state-of-art of aptamer-based antibacterial and antiviral therapeutic strategies. Diverse aptamers targeting pathogen-related components or who...
#1Xufen Yu (MSSM: Icahn School of Medicine at Mount Sinai)H-Index: 14
#2Jia Xu (MSSM: Icahn School of Medicine at Mount Sinai)H-Index: 45
Last. Jian Jin (MSSM: Icahn School of Medicine at Mount Sinai)H-Index: 51
view all 10 authors...
The serine/threonine kinase AKT functions as a critical node of the phosphatidylinositol 3-kinase (PI3K)/AKT/mammalian target of rapamycin (m-TOR) signaling pathway. Aberrant activation and overexpression of AKT are strongly correlated with numerous human cancers. To date, only two AKT degraders with no structure-activity relationship (SAR) results have been reported. Through extensive SAR studies on various linkers, E3 ligase ligands, and AKT binding moieties, we identified two novel and potent...
#1Xin He (CPU: China Pharmaceutical University)H-Index: 3
#2He Guangchao (CPU: China Pharmaceutical University)H-Index: 2
Last. Qihua Zhu (CPU: China Pharmaceutical University)H-Index: 12
view all 14 authors...
Indoleamine 2,3-dioxygenase-1 (IDO1) plays an important role in tumor immune escape. However, unsatisfactory clinical efficacies of selective IDO1 inhibitors have impeded their further development, suggesting that they do not exert sufficient antitumor effects by selectively inhibiting IDO1. IDO2, an isoenzyme of IDO1, is overexpressed in some human tumors, and emerging evidence suggests that concomitant inhibition of IDO1/2 may have synergistic effects in cancer treatment, revealing a promising...
#1Dongliang Guan (RTP: Research Triangle Park Foundation)
#2Toufiqur Rahman (RTP: Research Triangle Park Foundation)H-Index: 6
Last. Chunyang Jin (RTP: Research Triangle Park Foundation)H-Index: 11
view all 8 authors...
The central relaxin-3/RXFP3 system plays important roles in stress responses, feeding, and motivation for reward. However, exploration of its therapeutic applications has been hampered by the lack of small molecule ligands and the cross-activation of RXFP1 in the brain and RXFP4 in the periphery. Herein, we report the first structure-activity relationship studies of a series of novel nonpeptide amidinohydrazone-based agonists, which were characterized by RXFP3 functional and radioligand binding ...
#1Seung-Hwan KwonH-Index: 22
#2Sangjune KimH-Index: 15
Last. Han Seok KoH-Index: 30
view all 18 authors...
#1Wei Meng (BMS: Bristol-Myers Squibb)H-Index: 10
#2Zulan Pi (BMS: Bristol-Myers Squibb)H-Index: 8
Last. Heather Finlay (BMS: Bristol-Myers Squibb)H-Index: 13
view all 13 authors...
This paper describes our continued efforts in the area of small-molecule apelin receptor agonists. Recently disclosed compound 2 showed an acceptable metabolic stability but demonstrated monodemethylation of the dimethoxyphenyl group to generate atropisomer metabolites in vitro. In this article, we extended the structure-activity relationship at the C2 position that led to the identification of potent pyrazole analogues with excellent metabolic stability. Due to the increased polarity at C2, the...
#1Jintao Zhao (Lanzhou University)H-Index: 2
#2Zihua Wang (FJMU: Fujian Medical University)
Last. Jianguo Fang (Lanzhou University)H-Index: 38
view all 7 authors...
A diselenide/disulfide unit was introduced into camptothecin (CPT), and two selenoprodrugs (e.g., CPT-Se3 and CPT-Se4) were identified to show improved potency in killing cancer cells and inhibiting tumor growth in vivo. Interestingly, the intrinsic fluorescence of CPT was severely quenched by the diselenide bond. Both the selenoprodrugs were activated by glutathione with a nearly complete recovery of CPT's fluorescence. The activation of prodrugs was accompanied by the production of selenol int...
#1Zuojie Li (Liaocheng University)H-Index: 3
#2Qingpeng Wang (Liaocheng University)H-Index: 9
Last. Zhengping Wang (Liaocheng University)H-Index: 13
view all 10 authors...
Metastasis is a major contributor of death in cancer patients, and there is an urgent need for effective treatments of metastatic malignancies. Herein, ketoprofen (KP) and loxoprofen (LP) platinum(IV) complexes with antiproliferative and antimetastatic properties were designed and prepared by integrating chemotherapy and immunotherapy targeting cyclooxygenase-2 (COX-2), matrix metalloproteinase-9 (MMP-9), and programmed death ligand 1 (PD-L1), besides DNA. A mono-KP platinum(IV) complex with a c...
#1Xingchen Liu (CPU: China Pharmaceutical University)H-Index: 2
#2Cheng Wang (CPU: China Pharmaceutical University)H-Index: 10
Last. Ling-Yi Kong (CPU: China Pharmaceutical University)H-Index: 45
view all 12 authors...
As a vital kinase in the glycolysis system, PKM2 is extensively expressed in colorectal cancer (CRC) to support the energy and biosynthetic needs. In this study, we designed a series of parthenolide (PTL) derivatives through a stepwise structure optimization, and an excellent derivate 29e showed good activity on PKM2 (AC50 = 86.29 nM) and displayed significant antiproliferative activity against HT29 (IC50 = 0.66 μM) and SW480 (IC50 = 0.22 μM) cells. 29e decreased the expression of total PKM2, pr...
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