Search results for: Yongzhou Hu

Items from 1 to 20 out of 86 results

article

Discovery of a novel series of α-terpineol derivatives as promising anti-asthmatic agents: Their design, synthesis, and biological evaluation

Wanping Zhu, Xia Liu, Yuji Wang, Yeling Tong, more

European Journal of Medicinal Chemistry > 2018 > 143 > C > 419-425

A series of novel α-terpineol derivatives were designed and synthesized through structural derivatization of the tertiary hydroxyl moiety or reduction of the double bond. Of the resulting compounds, eight compounds enhanced relaxation of airway smooth muscle (ASM) compared to the α-terpineol precursor, and four compounds (4a, 4d, 4e, and 4i)were superior or comparable to aminophylline at a concentration...

article

A fluorogenic probe for imaging protein S-nitrosylation in live cells

Shiyi Shao, Bo Chen, Juan Cheng, Chengkun Wang, more

Biosensors and Bioelectronics > 2017 > 94 > C > 162-168

S-nitrosylation is a posttranslational modification of protein cysteine residues leading to the formation of S-nitrosothiols and its detection is crucial to understanding of redox regulation and NO-based signaling. Prototypical detection methods for S-nitrosylation are always carried out ex situ. However, the reversible nature and the tendency of transnitrosylation highlight the necessity of its probing...

article

Palladium‐Catalyzed, Silver‐Assisted Direct C‐5–H Arylation of 3‐Substituted 1,2,4‐Oxadiazoles under Microwave Irradiation

Shan Li, Penghui Wan, Jing Ai, Rong Sheng, more

Advanced Synthesis & Catalysis > 359 > 5 > 772 - 778

A direct C‐5–H arylation of 3‐substituted 1,2,4‐oxadiazoles with aryl iodides in the presence of a palladium catalyst and silver acetate is reported. This method provides a rapid, reliable way to obtain versatile 3,5‐diaryl‐1,2,4‐oxadiazole derivatives, which are common moieties of many biologically active molecules. The synthetic applications of this novel method have been demonstrated in the concise...

article

Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors

Jiankang Zhang, Xiaoqing Lv, Xiaodong Ma, Yongzhou Hu

European Journal of Medicinal Chemistry > 2017 > 127 > C > 509-520

Recently, the phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) have been considered as promising targets for the treatment of cancer. Herein, we synthesized a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as novel PI3K/mTOR dual inhibitors for cancer therapy. In the biological evaluation, compound 17e was identified as a potent PI3K/mTOR dual inhibitor, which...

article

Discovery of 4-chloro-3-(5-(pyridin-3-yl)-1,2,4-oxadiazole-3-yl)benzamides as novel RET kinase inhibitors

Mei Han, Shan Li, Jing Ai, Rong Sheng, more

Bioorganic & Medicinal Chemistry Letters > 2016 > 26 > 23 > 5679-5684

A series of novel 4-chloro-benzamides derivatives containing substituted five-membered heteroaryl ring were designed, synthesized and evaluated as RET kinase inhibitors for cancer therapy. Most of compounds exhibited moderate to high potency in ELISA-based kinase assay. In particular, compound I-8 containing 1,2,4-oxadiazole strongly inhibited RET kinase activity both in molecular and cellular level...

article

Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors

Wenhu Zhan, Lei Xu, Xiaowu Dong, Jun Dong, more

European Journal of Medicinal Chemistry > 2016 > 117 > C > 47-58

A series of novel pyrazol-furan carboxamide analogues were designed, synthesized and biologically evaluated for their Akt1 inhibitory activities, as well as anti-proliferative efficacies against HCT116 and OVCAR-8 cell lines. Most compounds exhibited moderate to excellent Akt1 inhibitory activities, together with favorable cytotoxicities. Further kinase selectivity assay of the most promising compound...

article

Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation

Xiaodong Ma, Xiaoqing Lv, Ni Qiu, Bo Yang, more

Bioorganic & Medicinal Chemistry > 2015 > 23 > 24 > 7585-7596

A series of quinoline derivatives featuring the novelty of introducing intra-molecular hydrogen bonding scaffold (iMHBS) were designed, synthesized and biologically evaluated for their mTOR inhibitory activity, as well as anti-proliferative efficacies against HCT-116, PC-3 and MCF-7 cell lines. As a result, six compounds exhibited significant inhibition against mTOR with IC₅₀ values below 35nM. Compound...

article

Design, synthesis and biological evaluation of novel 4-alkynyl-quinoline derivatives as PI3K/mTOR dual inhibitors

Xiaoqing Lv, Huazhou Ying, Xiaodong Ma, Ni Qiu, more

European Journal of Medicinal Chemistry > 2015 > 99 > Complete > 36-50

A novel series of 4-alkynyl-quinoline derivatives were designed, synthesized and biologically evaluated for their PI3Kα inhibitory activities and anti-proliferative effects against two cancer cell lines PC-3 and HCT-116. Most of them showed potent PI3Kα inhibitory activities with IC ₅₀ values at low nanomolar level and good to excellent anti-proliferative effects against both cell lines. Among...

article

Identification of novel inhibitors of Aurora A with a 3-(pyrrolopyridin-2-yl)indazole scaffold

Pinrao Song, Ming Chen, Xiaodong Ma, Lei Xu, more

Bioorganic & Medicinal Chemistry > 2015 > 23 > 8 > 1858-1868

A novel series of 3-(pyrrolopyridin-2-yl)indazole derivatives were synthesized and biologically evaluated for their anti-proliferative effects on five human cancer cell lines. As a result, all of them exhibited vigorous potency against HL60 cell line with IC ₅₀ values ranging from singe digital nanomolar to micromolar level. Besides, a majority of them displayed modest to good antiproliferative...

article

Mapping hydrogen sulfide in rats with a novel azo-based fluorescent probe

Xin Li, Juan Cheng, Yanling Gong, Bo Yang, more

Biosensors and Bioelectronics > 2015 > 65 > Complete > 302-306

We report herein a reaction-based fluorescent switch-on sulfide sensor, azo3, for the quantification of endogenous sulfides in rat tissues. The sensor was exploited based on the novel azo-sulfide chemistry and designed by locking the rhodol fluorophore into its nonfluorescent form with an azo group. However, the azo group would undergo a specific and biocompatible reaction with sulfides, triggering...

article

Design, synthesis, and biological evaluation of novel 2-methylpiperazine derivatives as potent CCR5 antagonists

Suwen Hu, Zhilong Wang, Tingjun Hou, Xiaodong Ma, more

Bioorganic & Medicinal Chemistry > 2015 > 23 > 5 > 1157-1168

Three series of novel 2-methylpiperazine derivatives were designed and synthesized using a fragment-assembly strategy. Among them, six compounds (13, 16, 18, 22, 33, and 36) showed potent activity against CCR5 comparable to that of the positive control, maraviroc, in calcium mobilization assay. Moreover, some compounds were selected and further tested for their antiviral activity in HIV-1 single cycle...

article

Identification of novel 4-anilinoquinazoline derivatives as potent EGFR inhibitors both under normoxia and hypoxia

Weiyan Cheng, Youting Yuan, Ni Qiu, Peng Peng, more

Bioorganic & Medicinal Chemistry > 2014 > 22 > 24 > 6796-6805

A novel series of 4-anilinoquinazoline derivatives (19a–19t) were designed and synthesized through incorporation of the 2-nitroimidazole moiety into the 4-anilinoquinazoline scaffold of EGFR inhibitors. The most promising compound 19h displayed potent EGFR inhibitory activity with the IC ₅₀ value of 0.47nM. It also strongly suppressed the proliferation of A549 and HT-29 cells with sub-micromolar...

article

Design, Synthesis and Biological Evaluation of Peptidyl Epoxyketone Proteasome Inhibitors Composed of β‐amino Acids

Jiankang Zhang, Mengmeng Han, Xiaodong Ma, Lei Xu, more

Chemical Biology & Drug Design > 84 > 5 > 497 - 504

A series of novel di‐ and tripeptidyl epoxyketone derivatives composed of β‐amino acids were designed, synthesized and evaluated for their proteasome inhibitory activities and anti‐proliferation activities against two multiple myeloma cell lines RPMI 8226 and NCI‐H929 and normal cells (peripheral blood mononucleated cells). Among these tested compounds, tripeptidyl analogues showed much more potent...

article

Design and total synthesis of Mannich derivatives of marine natural product lamellarin D as cytotoxic agents

Li Shen, Nan Xie, Bo Yang, Yongzhou Hu, more

European Journal of Medicinal Chemistry > 2014 > 85 > Complete > 807-817

Enlightened by the modification route from Camptothecin (CPT) to Topotecan and based on classical drug design theory, a series of Mannich derivatives of lamellarin D were designed and synthesized in 26–27 steps starting from vanillin and isovanilin. All synthesized compounds were then biologically evaluated for their in vitro anti-cancer activities and Topo I inhibitory activities. The results showed...

article

Design, synthesis and evaluation of rivastigmine and curcumin hybrids as site-activated multitarget-directed ligands for Alzheimer’s disease therapy

Yujie Li, Peng Peng, Li Tang, Yunzhen Hu, more

Bioorganic & Medicinal Chemistry > 2014 > 22 > 17 > 4717-4725

A series of novel 2-methoxy-phenyl dimethyl-carbamate derivatives were designed, synthesized and evaluated as site-activated MTDLs based on rivastigmine and curcumin. Most of them exhibited good to excellent AChE and BuChE inhibitory activities with sub-micromolar IC₅₀ values. Among all the compounds, 6a demonstrated the most potent AChE inhibition with IC₅₀ value of 0.097μM, which is about 20-fold...

article

Design, synthesis and biological evaluation of thienopyridinones as Chk1 inhibitors

Pinrao Song, Peng Peng, Mengmeng Han, Xianchao Cao, more

Bioorganic & Medicinal Chemistry > 2014 > 22 > 17 > 4882-4892

A series of thienopyridinone derivatives was designed and synthesized as inhibitors of checkpoint kinase 1 (Chk1). Most of them exhibited moderate to good Chk1 inhibitory activities. Among them, compounds 8q, 8t, and 8w with excellent Chk1 inhibitory activities (IC₅₀ values of 4.05, 6.23, and 2.33nM, respectively) displayed strong synergistic effects with melphalan, a DNA-damaging agent in the cell-based...

article

Design, synthesis and biological evaluation of novel tripeptidyl epoxyketone derivatives constructed from β-amino acid as proteasome inhibitors

Jiankang Zhang, Jiayi Cao, Lei Xu, Yubo Zhou, more

Bioorganic & Medicinal Chemistry > 2014 > 22 > 11 > 2955-2965

A series of novel tripeptidyl epoxyketone derivatives constructed from β-amino acid were designed, synthesized and evaluated as proteasome inhibitors. All target compounds were tested for their proteasome inhibitory activities and selected compounds were tested for their anti-proliferation activities against two multiple myeloma (MM) cell lines RPMI 8226 and NCI-H929. Among them, eleven compounds...

article

Cap-dependent translation initiation factor, eIF4E, is the target for Ouabain-mediated inhibition of HIF-1α

Ji Cao, Lingjuan He, Guanyu Lin, Chunqi Hu, more

Biochemical Pharmacology > 2014 > 89 > 1 > 20-30

Hypoxia-inducible factor 1 (HIF-1), a heterodimeric transcription factor that mediates the adaptation of tumor cells and tissues to the hypoxic microenvironment, has attracted considerable interest as a potential therapeutic target. Recently, HIF-1α has been recognized as the critical target of cardiac glycosides for cancer therapy, but the molecular mechanism of cardiac glycosides’ inhibition of...

article

Integrating docking scores, interaction profiles and molecular descriptors to improve the accuracy of molecular docking: Toward the discovery of novel Akt1 inhibitors

Wenhu Zhan, Daqiang Li, Jinxin Che, Liangren Zhang, more

European Journal of Medicinal Chemistry > 2014 > 75 > Complete > 11-20

A set of forty-seven Akt1 inhibitors was used for the development of molecular docking based QSAR model by using nonlinear regression. The integration of docking scores, key interaction profiles and molecular descriptors remarkably improved the accuracy of the QSAR models, providing reasonable statistical parameters (R _train ² = 0.948, R _test ² = 0.907 and Q _cv ²...

article

Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors

Tao Liu, Wenhu Zhan, Yanming Wang, Liangren Zhang, more

European Journal of Medicinal Chemistry > 2014 > 73 > Complete > 167-176

A series of diphenylmethylamine derivatives were rationally designed, synthesized and biologically evaluated. Most of them exhibited moderate to good Akt1 inhibitory activities, as well as promising anti-proliferative efficacy against cancer cell lines. Besides, molecular docking studies were carried out to probe their binding modes with Akt1. Further kinase selectivity studies of compound 22c were...

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Search results for: Yongzhou Hu

Discovery of a novel series of α-terpineol derivatives as promising anti-asthmatic agents: Their design, synthesis, and biological evaluation

A fluorogenic probe for imaging protein S-nitrosylation in live cells

Palladium‐Catalyzed, Silver‐Assisted Direct C‐5–H Arylation of 3‐Substituted 1,2,4‐Oxadiazoles under Microwave Irradiation

Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors

Discovery of 4-chloro-3-(5-(pyridin-3-yl)-1,2,4-oxadiazole-3-yl)benzamides as novel RET kinase inhibitors

Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors

Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation

Design, synthesis and biological evaluation of novel 4-alkynyl-quinoline derivatives as PI3K/mTOR dual inhibitors

Identification of novel inhibitors of Aurora A with a 3-(pyrrolopyridin-2-yl)indazole scaffold

Mapping hydrogen sulfide in rats with a novel azo-based fluorescent probe

Design, synthesis, and biological evaluation of novel 2-methylpiperazine derivatives as potent CCR5 antagonists

Identification of novel 4-anilinoquinazoline derivatives as potent EGFR inhibitors both under normoxia and hypoxia

Design, Synthesis and Biological Evaluation of Peptidyl Epoxyketone Proteasome Inhibitors Composed of β‐amino Acids

Design and total synthesis of Mannich derivatives of marine natural product lamellarin D as cytotoxic agents

Design, synthesis and evaluation of rivastigmine and curcumin hybrids as site-activated multitarget-directed ligands for Alzheimer’s disease therapy

Design, synthesis and biological evaluation of thienopyridinones as Chk1 inhibitors

Design, synthesis and biological evaluation of novel tripeptidyl epoxyketone derivatives constructed from β-amino acid as proteasome inhibitors

Cap-dependent translation initiation factor, eIF4E, is the target for Ouabain-mediated inhibition of HIF-1α

Integrating docking scores, interaction profiles and molecular descriptors to improve the accuracy of molecular docking: Toward the discovery of novel Akt1 inhibitors

Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors

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