Neurochemistry of aging. 2. Design, synthesis and biological evaluation of halomethyl analogs of choline with high affinity choline transport inhibitory activity

1991 ◽  
Vol 34 (7) ◽  
pp. 2031-2036 ◽  
Author(s):  
Jehangir S. Mistry ◽  
Donald J. Abraham ◽  
Alan P. Kozikowski ◽  
Israel Hanin
Keyword(s):  
Inhibitory Activity ◽  
Biological Evaluation ◽  
Choline Transport ◽  
Design Synthesis ◽  
High Affinity ◽  
Synthesis And Biological Evaluation

Design, synthesis and biological evaluation of 2-amino-N-(2-aminophenyl)thiazole-5-carboxamide derivatives as novel Bcr-Abl and histone deacetylase dual inhibitors

RSC Advances ◽  
2016 ◽  
Vol 6 (105) ◽  
pp. 103178-103184 ◽  
Author(s):  
Xin Chen ◽  
Shuang Zhao ◽  
Yichao Wu ◽  
Yadong Chen ◽  
Tao Lu ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Inhibitory Activity ◽  
Biological Evaluation ◽  
Design Approach ◽  
Design Synthesis ◽  
Dual Inhibitors ◽  
Synthesis And Biological Evaluation ◽  
Novel Design

A novel design approach: combination of Bcr-Abl and HDAC inhibitory activity in one molecule to produce dual inhibitors.

scholarly journals Design, synthesis and biological evaluation of 2,3-dihydroimidazo[1,2-c]quinazoline derivatives as novel phosphatidylinositol 3-kinase and histone deacetylase dual inhibitors

RSC Advances ◽  
2017 ◽  
Vol 7 (82) ◽  
pp. 52180-52186 ◽  
Author(s):  
Yichao Wu ◽  
Weichen Dai ◽  
Xin Chen ◽  
Aixin Geng ◽  
Yadong Chen ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Inhibitory Activity ◽  
Biological Evaluation ◽  
Design Approach ◽  
Phosphatidylinositol 3 Kinase ◽  
Design Synthesis ◽  
Dual Inhibitors ◽  
Quinazoline Derivatives ◽  
Synthesis And Biological Evaluation ◽  
Novel Design

A novel design approach by combination of PI3K and HDAC inhibitory activity in one molecule to produce dual inhibitors.

scholarly journals Design, synthesis, and biological evaluation of novel urolithins derivatives as potential phosphodiesterase II inhibitors

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Long Tang ◽  
Jianchun Jiang ◽  
Guoqiang Song ◽  
Yajing Wang ◽  
Ziheng Zhuang ◽  
...  
Keyword(s):  
Small Molecules ◽  
Inhibitory Activity ◽  
Structural Modification ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
H Nmr ◽  
Lead Compounds ◽  
Activity Test ◽  
Synthesis And Biological Evaluation ◽  
C Nmr

AbstractA series of urolithins derivatives were designed and synthesized, and their structures have been confirmed by 1H NMR, 13C NMR, and HR-MS. The inhibitory activity of these derivatives on phosphodiesterase II (PDE2) was thoroughly studied with 3-hydroxy-8-methyl-6H-benzo[C]chromen-6-one and 3-hydroxy-7,8,9,10-tetrahydro-6H-benzo[C] chromen-6-one as the lead compounds. The biological activity test showed that compound 2e had the best inhibitory activity on PDE2 with an IC50 of 33.95 μM. This study provides a foundation for further structural modification and transformation of urolithins to obtain PDE2 inhibitor small molecules with better inhibitory activity.

Design, synthesis and biological evaluation of (1,3-diphenyl-1H-pyrazol-4-yl) methyl benzoate derivatives as potential BRAFV600E inhibitors

RSC Advances ◽  
2014 ◽  
Vol 4 (95) ◽  
pp. 52702-52711 ◽  
Author(s):  
Ya-Juan Qin ◽  
Man Xing ◽  
Ya-Liang Zhang ◽  
Jigar A. Makawana ◽  
Ai-Qin Jiang ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Biological Evaluation ◽  
Methyl Benzoate ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Potent Inhibitory Activity ◽  
Benzoate Derivatives

A series of (1,3-diphenyl-1H-pyrazol-4-yl) methyl benzoate derivatives (6a–10d) were designed and synthesized and evaluated as BRAFV600 inhibitors. Among them, compound 10a showed the most potent inhibitory activity against A375, WM266.4 and BRAFV600Ein vitro with IC50 values of 1.36 μM, 0.94 μM and 0.11 μM, respectively.

Design, Synthesis, and Biological Evaluation of Small, High-Affinity Siglec-7 Ligands: Toward Novel Inhibitors of Cancer Immune Evasion

2017 ◽  
Vol 60 (3) ◽  
pp. 941-956 ◽  
Author(s):  
Horst Prescher ◽  
Martin Frank ◽  
Stephan Gütgemann ◽  
Elena Kuhfeldt ◽  
Astrid Schweizer ◽  
...  
Keyword(s):  
Immune Evasion ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
High Affinity ◽  
Synthesis And Biological Evaluation

scholarly journals Design, Synthesis, and Biological Evaluation of 1,2,3-Triazole-linked triazino[5,6-b]indole-benzene sulfonamide Conjugates as Potent Carbonic Anhydrase I, II, IX, and XIII Inhibitors

Metabolites ◽  
2020 ◽  
Vol 10 (5) ◽  
pp. 200
Author(s):  
Krishna Kartheek Chinchilli ◽  
Andrea Angeli ◽  
Pavitra S. Thacker ◽  
Laxman Naik Korra ◽  
Rashmita Biswas ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Inhibitory Activity ◽  
Biological Evaluation ◽  
Moderate Activity ◽  
Design Synthesis ◽  
Carbonic Anhydrase I ◽  
Potent Inhibition ◽  
Lead Candidate ◽  
Synthesis And Biological Evaluation ◽  
Nanomolar Range

A series of 1,2,3-triazole-linked triazino[5,6-b]indole-benzene sulfonamide hybrids (6a–6o) was synthesized and evaluated for carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity against the human (h) isoforms hCA I, II, XIII (cytosolic isoforms), and hCA IX (transmembrane tumor-associated isoform). The results revealed that the compounds 6a–6o exhibited Ki values in the low to medium nanomolar range against hCA II and hCA IX (Kis ranging from 7.7 nM to 41.3 nM) and higher Ki values against hCA I and hCA XIII. Compound 6i showed potent inhibition of hCA II (Ki = 7.7nM), being more effective compared to the standard inhibitor acetazolamide (AAZ) (Ki = 12.1 nM). Compounds 6b and 6d showed moderate activity against hCA XIII (Ki = 69.8 and 65.8 nM). Hence, compound 6i could be consider as potential lead candidate for the design of potent and selective hCA II inhibitors.

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