Abstract：
:Metal based therapeutics are a precious class of drugs in oncology research that include examples of theranostic drugs, which are active in both diagnostic, specifically imaging, and therapeutics applications. Ruthenium compounds have shown selective bioactivity and the ability to overcome the resistance that platinum-based therapeutics face, making them effective oncotherapeutic competitors in rational drug invention approaches. The development of antineoplastic ruthenium therapeutics is of particular interest because ruthenium containing complexes NAMI-A, KP1019, and KP1339 entered clinical trials and DW1/2 is in preclinical levels. The very robust, conformationally rigid organometallic Ru(II) compound DW1/2 is a protein kinase inhibitor and presents new Ru(II) compound designs as anticancer agents. Over the recent years, numerous strategies have been used to encapsulate Ru(II) derived compounds in a nanomaterial system, improving their targeting and delivery into neoplastic cells. A new photodynamic therapy based Ru(II) therapeutic, TLD-1433, has also entered clinical trials. Ru(II)-based compounds can also be photosensitizers for photodynamic therapy, which has proven to be an effective new, alternative, and noninvasive oncotherapy modality.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Thota S,Rodrigues DA,Crans DC,Barreiro EJdoi
10.1021/acs.jmedchem.7b01689subject
Has Abstractpub_date
2018-07-26 00:00:00pages
5805-5821issue
14eissn
0022-2623issn
1520-4804journal_volume
61pub_type
杂志文章,评审abstract：:A series of disubstituted ureas containing amide or amine groups was prepared and evaluated for their ability to inhibit acyl-CoA:cholesterol O-acyl transferase in vitro and to lower plasma total cholesterol in a variety of cholesterol-fed rat models in vivo. The presence of polar or ionizable functionalities within t...
journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
doi：10.1021/jm00038a010
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abstract：:The Free-Wilson equations are derived for the case of symmetrical substitution and are applied, in four modifications, to in vitro inhibitory activity of 77 organic disulfides against Histoplasma capsulatum. Substituent constants are listed to aid in the design of new inhibitory agents against this human pathogen (and...
journal_title：Journal of medicinal chemistry
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doi：10.1021/jm00238a004
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abstract：:Tropomyosin-related kinase A (TrkA) is considered a promising target in the development of a therapeutic treatment of cancer and pain. In this study, we designed and synthesized a series of novel 7-azaindole-based Trk kinase inhibitors through the structure-based design strategy. By varying the functional groups at th...
journal_title：Journal of medicinal chemistry
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journal_title：Journal of medicinal chemistry
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doi：10.1021/acs.jmedchem.5b00098
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journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
doi：10.1021/jm00219a017
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abstract：:Carbonates containing an iodinated aromatic ring on one side of the carbonate linkage and an alkyl group on the other were prepared. The aromatic side consisted of p-iodophenyl, p-iodobenzyl, m-iodobenzyl, 3,5-diiodobenzyl, m-amino-2,4,6-triiodobenzyl, m-acetamido-2,4,6-triiodobenzyl, p-iodophenethyl, p-iodo-sec-phene...
journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
doi：10.1021/jm00234a002
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journal_title：Journal of medicinal chemistry
pub_type： 杂志文章,评审
doi：10.1021/acs.jmedchem.0c00524
更新日期：2020-10-22 00:00:00
abstract：:Fatty acid amide hydrolase (FAAH), an intracellular serine hydrolase enzyme, participates in the deactivation of fatty acid ethanolamides such as the endogenous cannabinoid anandamide, the intestinal satiety factor oleoylethanolamide, and the peripheral analgesic and anti-inflammatory factor palmitoylethanolamide. In ...
journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
doi：10.1021/jm021119g
更新日期：2003-06-05 00:00:00
abstract：:N,N'-Diarylureas were prepared, and the structure-activity relationship relative to the CXCR2 receptor was examined. This led to the identification of a potent and highly selective CXCR2 antagonist, which in addition was shown to be functionally active both in vitro against human neutrophils and in vivo in rabbit mode...
journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
doi：10.1021/jm034248l
更新日期：2004-03-11 00:00:00
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journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
doi：10.1021/jm00099a004
更新日期：1992-10-16 00:00:00
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journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
doi：10.1021/acs.jmedchem.7b00530
更新日期：2018-02-08 00:00:00
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journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
doi：10.1021/jm00230a014
更新日期：1976-08-01 00:00:00
abstract：:Several N-2 substituted 1-methyl-1-(4-tolylsulfonyl)hydrazines were synthesized and evaluated for antineoplastic activity against the L1210 leukemia and the B16 melanoma. The most active compound to emerge from this study, 2-(methylsulfonyl)-1-methyl-1-(4-tolylsulfonyl)hydrazine, produced maximum percent T/C values wi...
journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
doi：10.1021/jm00157a033
更新日期：1986-07-01 00:00:00
abstract：:Gene therapy based on gene delivery is a promising strategy for the treatment of human disease. Here we present data on structure/biological activity of new biodegradable cholesterol-based cationic lipids with various heterocyclic cationic head groups and linker types. Enhanced accumulation of nucleic acids in the cel...
journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
doi：10.1021/jm901022t
更新日期：2009-11-12 00:00:00
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journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
doi：10.1021/jm00170a031
更新日期：1990-08-01 00:00:00
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journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
doi：10.1021/jm00106a003
更新日期：1991-02-01 00:00:00
abstract：:A series of tetrazole amide derivatives of (+/-)-2-dodecyl-alpha-phenyl-N-(2,4,6-trimethoxyphenyl)-2H-tetrazole-5- acetamide (1) was prepared and evaluated for their ability to inhibit acyl-CoA: cholesterol O-acyltransferase (ACAT) in vitro and to lower plasma total cholesterol in vivo. For this series of compounds, o...
journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
doi：10.1021/jm960170f
更新日期：1996-06-07 00:00:00
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journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
doi：10.1021/jm00353a004
更新日期：1982-11-01 00:00:00
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更新日期：2008-09-11 00:00:00
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journal_title：Journal of medicinal chemistry
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更新日期：2004-12-02 00:00:00
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journal_title：Journal of medicinal chemistry
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journal_title：Journal of medicinal chemistry
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更新日期：2018-09-13 00:00:00
abstract：:In a previous paper, we reported the N-hydroxyformamidine derivative HET0016 as a potent and selective 20-HETE synthase inhibitor. Despite its attraction as a potential therapeutic agent for cerebral diseases, the preparation of an injectable formulation of HET0016 was limited by its poor solubility under neutral cond...
journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
doi：10.1021/jm020557k
更新日期：2003-12-04 00:00:00
abstract：:Structure-based strategy was employed to design flavonoid compounds to mimic the Bim BH3 peptide as a new class of inhibitors of the anti-apoptotic Bcl-2 proteins. The most potent compound, 4 (BI-33), binds to Bcl-2 and Mcl-1 with Ki values of 17 and 18 nM, respectively. Compound 4 inhibits cell growth in the MDA-MB-2...
journal_title：Journal of medicinal chemistry
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更新日期：2007-07-12 00:00:00
