- Structural investigation into the inhibitory mechanisms of indomethacin and its analogues towards human glyoxalase I
[作者:Liu, M; Yuan, MG; Li, Z; Cheng, YK; Luo, HB; Hu, XP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4243-4247 , 文章类型: Article,,卷期:2011年21-14]
- In the present work, a combined study of kinetic analysis, molecular docking, and molecular dynamics simulations on indomethacin and its analogues is performed to better understand their inhibitory mechanisms towards hum...
- A transcription factor hijacking to regulate RAR alpha by using a chimeric molecule of retinoic acid and a DNA alkylator
[作者:Min, KH; Yun, BG; Lee, Y; Song, J; Ham, WH; Lee, Y; Park, HJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4248-4251 , 文章类型: Article,,卷期:2011年21-14]
- As a model compound for the transcription factor hijacking mechanism of action of DNA damaging agent that simultaneously bind to the nuclear receptor, we designed and synthesized a chimeric molecule, RA-mustard, which ca...
- Synthesis and evaluation of highly potent GABA(A) receptor antagonists based on gabazine (SR-95531)
[作者:Iqbal, F; Ellwood, R; Mortensen, M; Smart, TG; Baker, JR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4252-4254 , 文章类型: Article,,卷期:2011年21-14]
- A selection of highly potent analogues based on the gabazine structure is described. Their syntheses are carried out in just four steps, and their potencies for antagonism at the GABA(A) receptor were measured. All antag...
- Identification of non-amidine inhibitors of acid-sensing ion channel-3 (ASIC3)
[作者:Kuduk, SD; Chang, RK; Di Marco, CN; DiPardo, RM; Cook, SP; Cato, MJ; Jovanovska, A; Urban, MO; Leitl, M; Spencer, RH; Kane, SA; Hartman, GD; Bilodeau, MT,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4255-4258 , 文章类型: Article,,卷期:2011年21-14]
- A series of benzothiophene methyl amines were examined in an effort to identify non-amidine chemotypes with reduced polypharmacology from existing leads with the goal of finding potent ASIC3 channel blockers to advance t...
- In vitro inhibition of alpha-carbonic anhydrase isozymes by some phenolic compounds
[作者:Sarikaya, SBO; Topal, F; Senturk, M; Gulcin, I; Supuran, CT,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4259-4262 , 文章类型: Article,,卷期:2011年21-14]
- Carbonic anhydrase inhibitors (CAIs) are a class of pharmaceuticals used as antiglaucoma agents, diuretics, antiepileptics, in the management of mountain sickness, gastric and duodenal ulcers, neurological disorders or o...
- Anti-resorptive activity and pharmacokinetic study of N(1), N(1)-diisopropyl-N(2)-(diphenylphosphoryl)-2-(4-nitrophenyl) acetamidine
[作者:Kim, MH; Park, M; Song, JS; Park, SJ; Kim, SH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4263-4266 , 文章类型: Article,,卷期:2011年21-14]
- In vitro anti-resorptive activity, mechanism of action, pharmacokinetic profile and in vivo anti-resorptive activity of N(1),N(1)-diisopropyl-N(2)-(diphenylphosphoryl)-2-(4-nitrophenyl) acetamidine (1) were evaluated. (C...
- Pyrazoline based MAO inhibitors: Synthesis, biological evaluation and SAR studies
[作者:Jagrat, M; Behera, J; Yabanoglu, S; Ercan, A; Ucar, G; Sinha, BN; Sankaran, V; Basu, A; Jayaprakash, V,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4296-4300 , 文章类型: Article,,卷期:2011年21-14]
- Twenty-two pyrazoline derivatives were synthesized and tested for their human MAO (hMAO) inhibitory activity. Twelve molecules with unsubstituted ring A and substituted ring C (5-16) were found to be potent inhibitors of...
- Synthesis of some new 1,3,5-trisubstituted pyrazolines bearing benzene sulfonamide as anticancer and anti-inflammatory agents
[作者:Bashir, R; Ovais, S; Yaseen, S; Hamid, H; Alam, MS; Samim, M; Singh, S; Javed, K,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4301-4305 , 文章类型: Article,,卷期:2011年21-14]
- Thirteen new 2-pyrazoline derivatives bearing benzenesulfonamide moiety (2a-m) were synthesized by condensing appropriate chalcones with 4-hydrazinonbenzenesulfonamide hydrochloride and tested for anticancer and anti-inf...
- Pyrrolo[2,3-c]azepine derivatives: A new class of potent protein tyrosine phosphatase 1B inhibitors
[作者:Xie, JW; Tian, JY; Su, L; Huang, MN; Zhu, XH; Ye, F; Wan, YQ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4306-4309 , 文章类型: Article,,卷期:2011年21-14]
- A series of pyrrolo[2,3-c] azepine derivatives was designed, synthesized, and evaluated as a new class of inhibitors against protein tyrosine phosphatase 1B (PTP1B) in vitro. The results demonstrated that compounds beari...
- Synthesis and antitubercular evaluation of amidoalkyl dibenzofuranols and 1H-benzo[2,3]benzofuro[4,5-e][1,3]oxazin-3(2H)-ones
[作者:Kantevari, S; Yempala, T; Yogeeswari, P; Sriram, D; Sridhar, B,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4316-4319 , 文章类型: Article,,卷期:2011年21-14]
- A new class of amidoalkyl dibenzofuranols and 1H-benzo[2,3]benzofuro[4,5-e][1,3]oxazin-3(2H)-ones was synthesized in very good yields through polyphosphoric acid supported on silica (PPA-SiO(2)) catalyzed one-pot three c...
- Antihyperglycemic and neuroprotective effects of one novel Cu-Zn SOD mimetic
[作者:Wang, C; Li, S; Shang, DJ; Wang, XL; You, ZL; Li, HB,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4320-4324 , 文章类型: Article,,卷期:2011年21-14]
- Increasing evidence supports that OS plays important roles in diabetes mellitus and cerebral ischemia. This suggests that recovering an impaired endogenous superoxide dismutase (SOD) enzyme system induced by OS with a mi...
- Inhibition of a prolyl hydroxylase domain (PHD) by substrate analog peptides
[作者:Kwon, HS; Choi, YK; Kim, JW; Park, YK; Yang, EG; Ahn, DR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4325-4328 , 文章类型: Article,,卷期:2011年21-14]
- Oxygen dependent degradation of hypoxia-inducible factor (HIF)-1 alpha is triggered with hydroxylation by proline hydroxylase domain 2 (PHD2) under normoxic conditions. Some of previously developed PHD2 inhibitors show a...
- Synthesis and evaluation of chromenyl barbiturates and thiobarbiturates as potential antitubercular agents
[作者:Laxmi, SV; Reddy, YT; Kuarm, BS; Reddy, PN; Crooks, PA; Rajitha, B,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4329-4331 , 文章类型: Article,,卷期:2011年21-14]
- A novel series of barbiturate and thiobarbiturate analogs of 2-benzoyl-3-methyl-5-oxo-5H-furo[3,2-g] chromene-6-carbaldehydes (3a-g and 4a-d, respectively) and 6-methyl-4,8-dioxo-4,8-dihydropyrano[ 3,2-g] chromenes (7a-c...
- Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP
[作者:Gonzalez-Lopez, M; Welsh, K; Finlay, D; Ardecky, RJ; Ganji, SR; Su, Y; Yuan, HB; Teriete, P; Mace, PD; Riedl, SJ; Vuori, K; Reed, JC; Cosford, NDP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4332-4336 , 文章类型: Article,,卷期:2011年21-14]
- We report the systematic rational design and synthesis of new monovalent Smac mimetics that bind preferentially to the BIR2 domain of the anti-apoptotic protein XIAP. Characterization of compounds in vitro (including 9i;...
- Discovery of a new type inhibitor of human glyoxalase I by myricetin-based 4-point pharmacophore
[作者:Takasawa, R; Tao, A; Saeki, K; Shionozaki, N; Tanaka, R; Uchiro, H; Takahashi, S; Yoshimori, A; Tanuma, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4337-4342 , 文章类型: Article,,卷期:2011年21-14]
- The human glyoxalase I (hGLO I), which is a rate-limiting enzyme in the pathway for detoxification of apoptosis-inducible methylglyoxal (MG), has been expected as an attractive target for the development of new anti-canc...
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