Bioorganic & Medicinal Chemistry Letters
IF
2.44
Papers
27187
Papers 27112
1 page of 2,712 pages (27.1k results)
Newest
Published on Feb 1, 2019in Bioorganic & Medicinal Chemistry Letters 2.44
Ruolan Zhou (Wuhan Polytechnic University), Shaoyu Fang (Wuhan Polytechnic University)+ 8 AuthorsXin Chen1
Estimated H-index: 1
(Wuhan Polytechnic University)
Abstract Multiple myeloma (MM) is the second most common haematological malignancy. Almost all patients with MM eventually relapse, and most recommended treatment protocols for the patients with relapsed refractory MM comprise a combination of drugs with different mechanisms of action. Therefore novel drugs are in urgent need in clinic. Bcl-2 inhibitors and HDAC inhibitors were proved their anti-MM effect in clinic or under clinical trials, and they were further discovered to have synergistic in...
Source Cite
Published on Feb 1, 2019in Bioorganic & Medicinal Chemistry Letters 2.44
Jason Jacintho2
Estimated H-index: 2
,
Christopher Baccei13
Estimated H-index: 13
+ 11 AuthorsDaniel S. Lorrain19
Estimated H-index: 19
Abstract We previously published on the design and synthesis of novel, potent and selective PPARα antagonists suitable for either i.p. or oral in vivo administration for the potential treatment of cancer. Described herein is SAR for a subsequent program, where we set out to identify selective and potent PPARα/δ dual antagonist molecules. Emerging literature indicates that both PPARα and PPARδ antagonism may be helpful in curbing the proliferation of certain types of cancer. This dual antagonism ...
Source Cite
Published on Jan 1, 2019in Bioorganic & Medicinal Chemistry Letters 2.44
Jiadai Zhai (Shandong University of Technology), Lin Fu (Shandong University of Technology)+ 7 AuthorsFeng Sang (Shandong University of Technology)
Abstract Sanjuanolide, psorachalcone A and its seven new analogues were synthesized via a combinatorial strategy by aldol reaction. In order to investigate the effect between electron density in π-conjugated systems and biological activities, several electron-withdrawing and electron-donating groups were introduced at C-4 and the phenolic hydroxyl groups of sanjuanolide. The two natural products and its seven new analogues were investigated for their inhibitory effects against five cancer cell l...
Source Cite
Published on Jan 23, 2019in Bioorganic & Medicinal Chemistry Letters 2.44
Abstract In oncology, the “Warburg effect” describes the elevated production of energy by glycolysis in cancer cells. The ubiquitous and hypoxia-induced 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3) plays a noteworthy role in the regulation of glycolysis by producing fructose-2,6-biphosphate (F-2,6-BP), a potent activator of the glycolysis rate-limiting phosphofructokinase PFK-1. Series of amides and sulfonamides derivatives based on a N -aryl 6-aminoquinoxaline scaffold were sy...
Source Cite
Published on Apr 1, 2019in Bioorganic & Medicinal Chemistry Letters 2.44
Kai Cheng2
Estimated H-index: 2
(Hefei University of Technology),
Shiyu Li2
Estimated H-index: 2
(Hefei University of Technology)
+ 7 AuthorsChenzhong Liao12
Estimated H-index: 12
(Hefei University of Technology)
Abstract Herein we report our efforts of developing reversible selective hMAO-B inhibitors based on isatin, a fragment in an X-ray crystal structure. Five different scaffolds were designed and many compounds were synthesized. Among them, compound A3 demonstrated very high potency and isoform selectivity against hMAO-B, 11 and 13 times more potent (IC 50 = 3 nM) and 23.64 and 6.8 times more selective than the marked drugs, selegiline and safinamide. However, the endeavors to modify the polar 3-on...
1 Citations Source Cite
Published on Jan 1, 2019in Bioorganic & Medicinal Chemistry Letters 2.44
Binto Simon (University of Manchester), Claire Walmsley (University of Manchester)+ 4 AuthorsJohn M. Gardiner23
Estimated H-index: 23
(University of Manchester)
Abstract Synthetic neamine mimetics have been evaluated for binding to the HIV-1 Rev response element. Modified neamine derivatives, obtained from reductive amination of neamine, led to identification of new 6-amino modified neamine-type ligands with HIV-1 RRE binding affinity up to 20× that of neamine and up to 6× that of the more complex neomycin itself. This provides a noteworthy structure-activity increase and a useful lead to simplified, chemically accessible mimetics.
Source Cite
Published on Apr 1, 2019in Bioorganic & Medicinal Chemistry Letters 2.44
Hongna Wu3
Estimated H-index: 3
(Peking Union Medical College),
Jun Wu11
Estimated H-index: 11
(Chinese Academy of Sciences)
+ 7 AuthorsSong Wu5
Estimated H-index: 5
(Peking Union Medical College)
Abstract Aberrant Wnt signaling has been implicated in a variety of disease. Inhibition of the Wnt pathway is an attractive approach for developing new therapeutics for the treatment of various types of fibrosis and cancers. We have discovered the phthalimide-phenylpyridine conjugate as a novel hit compound for the Wnt pathway inhibitors from cellular screening. The structure-activity relationship of these compounds suggested both of the substituent group on the phthalimide fragment and the stru...
Source Cite
Published on Jan 1, 2019in Bioorganic & Medicinal Chemistry Letters 2.44
Jia-Hao Feng1
Estimated H-index: 1
(China Pharmaceutical University),
Xiao-Long Hu2
Estimated H-index: 2
(China Pharmaceutical University)
+ 6 AuthorsHao Wang10
Estimated H-index: 10
(China Pharmaceutical University)
Abstract • In this study, seven clovamide analogues ( 1 – 7 ) were designed and synthesized, and the neuroprotection of 1 – 7 as well as 8 – 15 (prepared in our previous work) against H 2 O 2 -induced oxidative stress was evaluated in SH-SY5Y cells. Results showed that 1 – 7 with catechol groups exhibited better neuroprotective effects than 8 – 15 , and their EC 50 values ranged from 4.26 to 23.83 μM, especially 1 , indicating that the moiety of catechol governed the activities of these compound...
Source Cite
Published on Apr 1, 2019in Bioorganic & Medicinal Chemistry Letters 2.44
Kazutaka Ikegashira2
Estimated H-index: 2
(Japan Tobacco),
Taku Ikenogami1
Estimated H-index: 1
(Japan Tobacco)
+ 7 AuthorsHiromasa Hashimoto8
Estimated H-index: 8
(Japan Tobacco)
Abstract Optimization of novel azetidine compounds, which we had found as colony stimulating factor-1 receptor (CSF-1R) Type II inhibitors, provided JTE-952 as a clinical candidate with high cellular activity (IC 50 = 20 nM) and good pharmacokinetics profile. JTE-952 was also effective against a mouse collagen-induced model of arthritis (mouse CIA-model). Additionally, the X-ray co-crystal structure of JTE-952 with CSF-1R protein was shown to be a Type II inhibitor, and the kinase panel assay in...
Source Cite
Published on Mar 1, 2019in Bioorganic & Medicinal Chemistry Letters 2.44
Chowdhury Raihan Bikash1
Estimated H-index: 1
(University of Nevada, Reno),
Yftah Tal-Gan12
Estimated H-index: 12
(University of Nevada, Reno)
Abstract Quorum sensing (QS) controls the pathogenic behavior of Streptococcus mutans , a primary cause of dental caries. S. mutans uses the competence stimulating peptide (CSP) to control mutacin production, a bacteriocin utilized by S. mutans to outcompete different commensal bacteria in mixed biofilm environments. In this study, we performed an N -methyl scan of an 18-CSP-based scaffold lacking the first two amino acid residues that were shown to be dispensable, to gain important mechanistic ...
Source Cite
12345678910