Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation

Xiaodong Ma; Fang Fang; Qiangqiang Tao; Li Shen; Guochen Zhong; Tao Qiao; Xiaoqing Lv; Jiaming Li

doi:10.1039/c8md00556g

Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation

MedChemComm ◽

10.1039/c8md00556g ◽

2019 ◽

Vol 10 (3) ◽

pp. 413-420 ◽

Cited By ~ 2

Author(s):

Xiaodong Ma ◽

Fang Fang ◽

Qiangqiang Tao ◽

Li Shen ◽

Guochen Zhong ◽

...

Keyword(s):

Biological Evaluation ◽

Selective Inhibitors ◽

Conformational Restriction ◽

Design Synthesis ◽

Conformationally Restricted ◽

Synthesis And Biological Evaluation

A series of structurally novel quinazolone-based PI3Kδ-selective inhibitors were designed and synthesized via the approach of conformational restriction.

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Design, synthesis, and biological evaluation of novel (1-thioxo-1,2,3,4-tetrahydro-β-carbolin-9-yl)acetic acids as selective inhibitors for AKR1B1

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2011.10.073 ◽

2012 ◽

Vol 20 (1) ◽

pp. 356-367 ◽

Cited By ~ 8

Author(s):

Daisuke Minehira ◽

Daisuke Takeda ◽

Hirokazu Urata ◽

Atsushi Kato ◽

Isao Adachi ◽

...

Keyword(s):

Biological Evaluation ◽

Selective Inhibitors ◽

Design Synthesis ◽

Synthesis And Biological Evaluation ◽

Acetic Acids

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Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2019.03.005 ◽

2019 ◽

Vol 170 ◽

pp. 112-125 ◽

Cited By ~ 3

Author(s):

Xiaodong Ma ◽

Jun Wei ◽

Chang Wang ◽

Dongyan Gu ◽

Yongzhou Hu ◽

...

Keyword(s):

B Cell ◽

Biological Evaluation ◽

Selective Inhibitors ◽

Design Synthesis ◽

Synthesis And Biological Evaluation

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Design, synthesis and biological evaluation of trinary benzocoumarin-thiazoles-azomethines derivatives as effective and selective inhibitors of alkaline phosphatase

Bioorganic Chemistry ◽

10.1016/j.bioorg.2019.103137 ◽

2019 ◽

Vol 91 ◽

pp. 103137 ◽

Cited By ~ 5

Author(s):

Pervaiz Ali Channar ◽

Hina Irum ◽

Abid Mahmood ◽

Ghulam Shabir ◽

Sumera Zaib ◽

...

Keyword(s):

Alkaline Phosphatase ◽

Biological Evaluation ◽

Selective Inhibitors ◽

Design Synthesis ◽

Synthesis And Biological Evaluation

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Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2017.08.029 ◽

2018 ◽

Vol 26 (8) ◽

pp. 1418-1425 ◽

Cited By ~ 6

Author(s):

Jinyu Yang ◽

Gaoliang Cheng ◽

Qihao Xu ◽

Shenglin Luan ◽

Shuxiang Wang ◽

...

Keyword(s):

Histone Deacetylase ◽

Hydroxamic Acid ◽

Biological Evaluation ◽

Histone Deacetylase 6 ◽

Selective Inhibitors ◽

Design Synthesis ◽

Recognition Motif ◽

Surface Recognition ◽

Synthesis And Biological Evaluation

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Design, synthesis, and biological evaluation of human sialidase inhibitors. Part 1: Selective inhibitors of lysosomal sialidase (NEU1)

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2007.11.084 ◽

2008 ◽

Vol 18 (2) ◽

pp. 532-537 ◽

Cited By ~ 41

Author(s):

Sadagopan Magesh ◽

Setsuko Moriya ◽

Tohru Suzuki ◽

Taeko Miyagi ◽

Hideharu Ishida ◽

...

Keyword(s):

Biological Evaluation ◽

Selective Inhibitors ◽

Design Synthesis ◽

Synthesis And Biological Evaluation ◽

Lysosomal Sialidase

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Design, Synthesis, and Biological Evaluation of Orally Available First-Generation Dual-Target Selective Inhibitors of Acetylcholinesterase (AChE) and Phosphodiesterase 5 (PDE5) for the Treatment of Alzheimer’s Disease

ACS Chemical Neuroscience ◽

10.1021/acschemneuro.7b00345 ◽

2017 ◽

Vol 9 (2) ◽

pp. 328-345 ◽

Cited By ~ 21

Author(s):

Fei Mao ◽

Huan Wang ◽

Wei Ni ◽

Xinyu Zheng ◽

Manjiong Wang ◽

...

Keyword(s):

Alzheimer’S Disease ◽

Alzheimer's Disease ◽

First Generation ◽

Biological Evaluation ◽

Selective Inhibitors ◽

Design Synthesis ◽

Synthesis And Biological Evaluation ◽

Phosphodiesterase 5 ◽

Dual Target

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Design, Synthesis, and Biological Evaluation of Conformationally Restricted Rivastigmine Analogues

Journal of Medicinal Chemistry ◽

10.1021/jm049782n ◽

2004 ◽

Vol 47 (24) ◽

pp. 5945-5952 ◽

Cited By ~ 92

Author(s):

Maria Laura Bolognesi ◽

Manuela Bartolini ◽

Andrea Cavalli ◽

Vincenza Andrisano ◽

Michela Rosini ◽

...

Keyword(s):

Biological Evaluation ◽

Design Synthesis ◽

Conformationally Restricted ◽

Synthesis And Biological Evaluation

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Design, synthesis and biological evaluation of new tryptamine and tetrahydro-β-carboline-based selective inhibitors of CDK4

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2008.07.002 ◽

2008 ◽

Vol 16 (16) ◽

pp. 7728-7739 ◽

Cited By ~ 37

Author(s):

Paul R. Jenkins ◽

James Wilson ◽

Daniel Emmerson ◽

Marcos D. Garcia ◽

Matthew R. Smith ◽

...

Keyword(s):

Biological Evaluation ◽

Selective Inhibitors ◽

Design Synthesis ◽

Synthesis And Biological Evaluation

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Conformationally Restricted Hybrid Analogues of the Hormone 1α,25-Dihydroxyvitamin D3: Design, Synthesis, and Biological Evaluation

Bioorganic & Medicinal Chemistry ◽

10.1016/s0968-0896(01)00087-6 ◽

2001 ◽

Vol 9 (7) ◽

pp. 1691-1699 ◽

Cited By ~ 5

Author(s):

M.Christina White ◽

Martin D Burke ◽

Sara Peleg ◽

Henry Brem ◽

Gary H Posner

Keyword(s):

Biological Evaluation ◽

Dihydroxyvitamin D3 ◽

Design Synthesis ◽

Conformationally Restricted ◽

Synthesis And Biological Evaluation

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The Orientation of the TerminaltBu Group of Antillatoxin is Important for Potent Toxicity: Design, Synthesis and Biological Evaluation of Conformationally Restricted Analogues of Antillatoxin

Asian Journal of Organic Chemistry ◽

10.1002/ajoc.201300111 ◽

2013 ◽

Vol 2 (8) ◽

pp. 650-653 ◽

Cited By ~ 3

Author(s):

Ken Okura ◽

Masayuki Inoue

Keyword(s):

Biological Evaluation ◽

Design Synthesis ◽

Conformationally Restricted ◽

Synthesis And Biological Evaluation

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