Synthesis and biological evaluation of imidazo[4,5-b]pyridine and 4-heteroaryl-pyrimidine derivatives as anti-cancer agents

Łukasik, Paweł; Elabar, Sherifa; Lam, Frankie; Shao, Hao; Liu, Xiangrui; Abbas, Abdullah Y.; Wang, Shudong

doi:10.1016/j.ejmech.2012.09.034

Cited by 71 publications

(47 citation statements)

References 14 publications

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“…Among the various fused systems, pyrazolopyridines show promising biological activities as antibacterial [2], antitumor [3], antiviral [4] and anti-inflammatory [5] agents, and antagonists of corticotropin-releasing factor 1 (CRF 1 ) [6], chemokine receptor type 1 (CCR1) [7] and dopamine D3 receptors antagonists [8]. They are also known to be cholesterol forming [9], acetyl-CoA carboxylase (ACC) [10], HIV reverse transcriptase [11], phosphodiesterase 3/4 (PDE3/4) cyclin-dependent 1 (CDK1) [12], and B-Raf kinase inhibitors [13]. Several methods have been devised for the synthesis of substituted pyrazolopyridines [14][15][16][17][18][19][20].…”

Section: Introductionmentioning

confidence: 99%

Three-component one-pot synthesis of dihydrochromeno[4,3-b]pyrazolo[4,3-e]pyridines

Sadat-Ebrahimi

Katebi

Pirali-Hamedani

et al. 2016

Heterocyclic Communications

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Section: Introductionmentioning

confidence: 99%

Three-component one-pot synthesis of dihydrochromeno[4,3-b]pyrazolo[4,3-e]pyridines

Sadat-Ebrahimi

Katebi

Pirali-Hamedani

et al. 2016

Heterocyclic Communications

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“…[13] Derivatives of N-phenyl-imidazo [4,5-b] pyridin-2-amines, 4-indazolyl-N-phenylpyrimidin-2-amines and Nphenyl-4-pyrazolo [3,4-b] pyridin-pyrimidin-2-amines [ Table-2] were used as potent anti-proliferative and CDK9 inhibitory activities in the present study. [14] Table 3 identifies the evaluated ADME physico chemical properties of all ligands under study. The property of each ligand was calculated in order to identify any ligand violating Lipinski rule of 5.…”

Section: Dataset Selectionmentioning

confidence: 99%

Virtual Screening of CDK9 Inhibitors as Potential Anti Cancer Drugs

Kumar¹,

Giri²,

Nadendla³

2017

IJCA

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Cell cycle inhibition is important hallmark of anti cancer research. CDKs are divided into two types based on their Cell cycle controlling and transcriptional control. CDK 9, a transcriptional regulator serves as potential drug target. Only few drugs are under clinical trials phase 1/2/3 of CDK 9 inhibitory potential. 3BLR (pdb id) is used as docking target. Virtual screening is carried out based on the pharmacophore information generated from literature. Docking is carried out using Molegro virtual docker with all the compounds and top ranking compounds are shortlisted. The best compound (ZINC91643349) was identified and further analyzed by Invitro assays.

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“…Their activities include anti-cancer (Lukasik et al, 2012), antiviral (Cristalli, et al, 1995) and antimitotic (Aridoss et al, 2006) actions.…”

Section: Structure Descriptionmentioning

confidence: 99%

6-Bromo-2-methyl-1H-imidazo[4,5-b]pyridine

Bouayad

Rodi²,

Ghadraoui

et al. 2016

IUCr Data

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The title molecule, C 7 H 6 BrN 3 , crystallizes with two molecules, A and B, in the asymmetric unit, with all non-hydrogen atoms lying on a crystallographic mirror plane. In the crystal, the molecules are linked into [100] chains of alternating A and B molecules by complementary N-HÁ Á ÁN and C-HÁ Á ÁN hydrogen bonds. The chains are associated through offset aromatic -stacking [shortest centroid-centroid separation = 3.6215 (9) In this study, we have reacted 3-acetyl-4-hydroxy-6-methyl-3H-pyran-2-one (dehydroacetic acid) with 5-bromopyridine-2,3-diamine to furnish the title compound 6-bromo-2-methyl-1H-imidazo [4,5-b]pyridineÁThe asymmetric unit (Fig. 1) consists of two molecules, each lying on a crystallographic mirror plane.In the crystal, complementary pairs of N2-H2Á Á ÁN4 and C3-H3Á Á ÁN5 as well as N6-H6Á Á ÁN1 i and C10-H10Á Á ÁN3 i [symmetry code: (i) x À 1, y, z] hydrogen bonds (Table 1) form chains running parallel to the a axis. These ribbons form stacks in the b-axis direction which are associated through offset -stacking with an average interplanar spacing of 3.236 (1) Å (Fig. 2).

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Synthesis and biological evaluation of imidazo[4,5-b]pyridine and 4-heteroaryl-pyrimidine derivatives as anti-cancer agents

Cited by 71 publications

References 14 publications

Three-component one-pot synthesis of dihydrochromeno[4,3-b]pyrazolo[4,3-e]pyridines

Three-component one-pot synthesis of dihydrochromeno[4,3-b]pyrazolo[4,3-e]pyridines

Virtual Screening of CDK9 Inhibitors as Potential Anti Cancer Drugs

6-Bromo-2-methyl-1H-imidazo[4,5-b]pyridine

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