Abstract:
:Several known alpha-amino acid analogues and a new compound, N-chloroacetylphosphoramidate, a carbamyl phosphate analogue, were screened as antitumor agents. All gave 50% growth inhibition of cultures of human epidemeroid carcinoma of the nasopharynx at dosage levels of 2-8 mug/ml while showing no activity against L1210 lymphoid leukemia in vivo in BDFi mice.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Glover GI,Nelson SO,Kaeder GRdoi
10.1021/jm00213a026subject
Has Abstractpub_date
1977-03-01 00:00:00pages
452-3issue
3eissn
0022-2623issn
1520-4804journal_volume
20pub_type
杂志文章abstract::The endocannabinoid 2-arachidonoylglycerol (2-AG) plays a major role in many physiological processes, and its action is quickly terminated via enzymatic hydrolysis catalyzed by monoglyceride lipase (MGL). Regulating its endogenous level could offer therapeutic opportunities; however, few selective MGL inhibitors have ...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm900461w
更新日期:2009-12-10 00:00:00
abstract::Ac-Tyr298-Ala299-Gly300-Thr301-Val302-I le303-Asn304-Asp305-Leu306-OH (Ac-VZV R2-(298-306)) represents the acetylated form of the C-terminus of varicella-zoster virus (VZV) ribonucleotide reductase subunit 2 (R2). This peptide possesses a high degree of homology with the C-terminus nonapeptide of the herpes simplex vi...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00080a021
更新日期:1992-01-24 00:00:00
abstract::As described in the preceding paper (Arvanitis et al. J. Med. Chem. 1999, 42), anilinopyrimidines I were identified as potent antagonists of corticotropin-releasing hormone-1 receptor (CRH1-R, also referred to as corticotropin-releasing factor, CRF1-R). Our next goal was to understand the receptor-bound conformation o...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm980223o
更新日期:1999-03-11 00:00:00
abstract::The human brain is a uniquely complex organ, which has evolved a sophisticated protection system to prevent injury from external insults and toxins. Designing molecules that can overcome this protection system and achieve optimal concentration at the desired therapeutic target in the brain is a specific and major chal...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章,评审
doi:10.1021/jm501535r
更新日期:2015-03-26 00:00:00
abstract::Based on the known biological activity of a variety of guanidine-containing agents, several N-substituted 3,4-dihydroquinazolines were synthesized. These compounds can be considered to be rigid analogues of phenylguanidines. In anesthetized rats the compounds decreased blood pressure and were antagonists of the presso...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00185a026
更新日期:1980-11-01 00:00:00
abstract::We have previously shown [Cys-Trp-Arg-Nva-Arg-Tyr-NH(2)](2), 1, to be a moderately selective neuropeptide Y (NPY) Y(4) receptor agonist. Toward improving the selectivity and potency for Y(4) receptors, we studied the effects of dimerizing H-Trp-Arg-Nva-Arg-Tyr-NH(2) using various diamino-dicarboxylic acids containing ...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm050907d
更新日期:2006-04-20 00:00:00
abstract::A series of novel cephalosporin compounds which have 3-[(aminopyrimidiniumyl)thio]methyl substituents was synthesized. They show high antimicrobial activity against various bacterial species including Pseudomonas aeruginosa. Structure-activity relationships with various thiopyrimidines, thiopyrimidiniums, bicyclic thi...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00048a018
更新日期:1994-10-28 00:00:00
abstract::The synthesis and in vitro and in vivo antibreast and antiprostate cancers activities of novel C-4 heteroaryl 13-cis-retinamides that modulate Mnk-eIF4E and AR signaling are discussed. Modifications of the C-4 heteroaryl substituents reveal that the 1H-imidazole is essential for high anticancer activity. The most pote...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm501792c
更新日期:2015-02-26 00:00:00
abstract::A series of 2- and 3-aminobenzanilides derived from ring-alkylated anilines were prepared and evaluated for anticonvulsant activity. These benzanilides were prepared in the course of studies designed to determine the relationship between the benzamide structure and anticonvulsant effects. The compounds were tested in ...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00158a038
更新日期:1986-08-01 00:00:00
abstract::N(α)-Boc-l-Asp(OBn)-l-Lys(Z)-OtBu (reversin 121, 1), an inhibitor of the P-gp ABC transporter, was used to conceive compounds inhibiting the drug efflux occurring through the Hoechst 33342 and daunorubicin transport sites of P-gp, respectively H and R sites. Replacement of the aspartyl residue by trans-4-hydroxy-l-pro...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm100839w
更新日期:2010-09-23 00:00:00
abstract::9-acridinyl derivatives of 1,6-hexanediamine, 1,8-octanediamine, bis(3-aminopropyl)amine, N,N'-bis(3-amino-propyl)piperazine, and N-ethyl-1,6-hexanediamine in the form of their hydrochlorides were prepared in high yields and converted into potential hetero bis DNA intercalating diacridines. The corresponding potential...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00364a028
更新日期:1983-10-01 00:00:00
abstract::Described in this paper is the synthesis and pharmacological activity of five metabolites of the angiotensin II antagonist tasosartan (1). Of particular interest is the effect of the additional acidic group of the enol metabolite (8) on activity. As suggested by the structural-activity relationship of other angiotensi...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm970690q
更新日期:1998-10-22 00:00:00
abstract::The cyclic AMP phosphodiesterase (cAMP PDE) inhibitor and cardiotonic agent lixazinone (N-cyclohexyl-N-methyl-4-[(1,2,3,5-tetrahydro-2- oxoimidazo[2,1-b]quinazolin-7-yl)oxy]butyramide, RS-82856, 1) and its acid and base addition salts were found to be insufficiently soluble in formulations suitable for intravenous adm...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00119a015
更新日期:1988-11-01 00:00:00
abstract::The conformation of the sodium salt of mycophenolic acid (MPA), a potent inhibitor of inosine monophosphate dehydrogenase (IMPD), derived from 1D DIFNOE and 2D ROESY experiments in water and molecular dynamics (MD) is described. The hexenoic acid side chain conformation consistent with the NMR data was similar to that...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm950600m
更新日期:1996-03-15 00:00:00
abstract::The steroidal sulfonylpyrazole 1 bound to the rat ventral prostate androgen receptor in vitro; it inhibited testosterone propionate induced increases in ventral prostate weight in vivo in the castrated, immature male rat with an ED50 of 15 mg/kg po. Compound 1 lacked androgenic activity in vivo in contrast to the pare...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00170a008
更新日期:1990-08-01 00:00:00
abstract::A series of UTP, UDP, and UMP derivatives and analogues were synthesized and evaluated at the human pyrimidinergic P2Y receptor subtypes P2Y2, P2Y4, and P2Y6 stably expressed in 1321N1 astrocytoma cells. Substituents at N3 of UTP were poorly tolerated by P2Y2 and P2Y4 receptors. In contrast, a large phenacyl substitue...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm060848j
更新日期:2006-11-30 00:00:00
abstract::The in vitro antineoplastic activity of many phosphorus-containing (e.g., phosphocholines) and non-phosphorus-containing (e.g., quaternary ammonium salts) ether lipids has been evaluated in the HL-60 promyelocytic cell line. These compounds are analogues of ET-18-OMe (1-O-octadecyl-2-O-methyl-rac-glycero-3-phosphochol...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00066a011
更新日期:1993-07-09 00:00:00
abstract::5-Alkoxy-3-(N-substituted carbamoly)-1-phenylpyrazoles were prepared and tested for antiinflammatory and hypnotic activity. Four compounds showed antiinflammatory activity and three possessed hypnotic properties. ...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00211a016
更新日期:1977-01-01 00:00:00
abstract::Benzocycloalkyl and benzocycloalkenyl moities linked, directly or via an alkyl chain, to oxygen-bearing heteroarylpiperazines were synthesized, in an attempt to obtain potent and selective antagonists at postsynaptic 5-HT1A receptors. From the numerous arylpiperazines described in the literature, 1-(2,3-dihydro-1,4-be...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00020a020
更新日期:1995-09-29 00:00:00
abstract::Intrigued by the role of protein acetylation in hepatitis C virus (HCV) replication, we tested known histone deacetylase (HDAC) inhibitors and a focused library of structurally simple hydroxamic acids for inhibition of a HCV subgenomic replicon. While known HDAC inhibitors with varied inhibitory profiles proved to be ...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm501330g
更新日期:2015-01-22 00:00:00
abstract::Human African trypanosomiasis is causing thousands of deaths every year in the rural areas of Africa. In this manuscript we describe the optimization of a family of phtalazinone derivatives. Phosphodiesterases have emerged as attractive molecular targets for a novel treatment for a variety of neglected parasitic disea...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/acs.jmedchem.9b00985
更新日期:2020-04-09 00:00:00
abstract::Endomorphin-2 (EM-2: Tyr-Pro-Phe-Phe-NH(2)) is an endogenous tetrapeptide that combines potency and efficacy with high affinity and selectivity toward the μ opioid receptor, the most responsible for analgesic effects in the central nervous system. The presence of the Pro(2) represents a crucial factor for the ligand s...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm201402v
更新日期:2012-04-12 00:00:00
abstract::Inherently conducting polymers (ICPs) are a specific category of synthetic polymers with distinctive electro-optic properties, which involve conjugated chains with alternating single and double bonds. Polyaniline (PANI), as one of the most well-known ICPs, has outstanding potential applications in biomedicine because ...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章,评审
doi:10.1021/acs.jmedchem.9b00803
更新日期:2020-01-09 00:00:00
abstract::Lofexidine, an alpha 2-agonist, has central hypotensive activity and peripheral intestinal antisecretory activity. Analogues were synthesized with increased polarity in an attempt to prevent penetration of the blood-brain barrier. The compounds were evaluated in the cholera toxin treated ligated jejunum of the rat and...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00164a024
更新日期:1990-02-01 00:00:00
abstract::A series of 5-substituted tetrahydroisoquinolines was synthesized via a 10-step linear synthesis to assess whether replacement of noscapine's southern isobenzofuranone with other moieties resulted in retained cytotoxic activity. One such molecule, 18g, bearing a para-methoxybenzyl functionality with N-ethylcarbamoyl s...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/acs.jmedchem.8b00986
更新日期:2018-09-27 00:00:00
abstract::Two new analogues derived from the platelet activating factor (PAF), containing glucosamine instead of the acetyl group, were synthesized, and their effect on the human keratinocyte cell line HaCaT was evaluated with respect to cytotoxicity, proliferation, adhesion, and migration. Starting with (R)-1,2-isopropylideneg...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm050558n
更新日期:2005-10-20 00:00:00
abstract::The synthesis and testing of potential multisubstrate inhibitors of tyrosine-specific protein kinases are described. One of the substrates, ATP, was mimicked by the known kinase inhibitor 5'-[4-(fluorosulfonyl)benzoyl]adenosine, which was covalently linked via the sulfonyl moiety to tyrosine mimics. The resulting mult...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00117a015
更新日期:1988-09-01 00:00:00
abstract::Optimization of the pharmacokinetic properties for a series of benzoxazolone derivatives led to the identification of 9b, which showed anxiolytic effect in a rat model. However, 9b, like known benzodiazepines, induced motor impairment. Investigation into the cause of this unexpected side effect and management of 9b of...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm401325r
更新日期:2013-10-24 00:00:00
abstract::The tetrapeptide H-Arg-Gly-Asp-Ser-OH (1) (RGDS), representing a recognition sequence of fibrinogen for its platelet receptor GP IIb-IIIa (integrin alpha IIb beta 3), served as lead compound for the development of highly potent and selective fibrinogen receptor antagonists. Replacement of the N-terminal arginine by p-...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00101a017
更新日期:1992-11-13 00:00:00
abstract::A series of novel tetrahydropyridinecarboxamide TRPV1 antagonists were prepared and evaluated in an effort to optimize properties of previously described lead compounds from piperazinecarboxamide series. The compounds were evaluated for their ability to block capsaicin and acid-induced calcium influx in CHO cells expr...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm500818a
更新日期:2014-08-14 00:00:00