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Discovery of novel CDK9 inhibitor for acute myeloid leukemia

Discovery of novel CDK9 inhibitor for acute myeloid leukemia

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Aoli Wang Chen Hu Hong Wu Ziping Qi Jing Liu Qingsong Liu High Magnetic Field Laboratory Chinese Academy of Sciences University of Science and Technology of China Precision Targeted Therapy Discovery Center Institute of Technology InnovationHefei Institutes of Physical ScienceChinese Academy of Sciences

Acute myeloid leukemia（AML） is heterogeneous hematologic malignancy,characterized by the rapid growth of abnormal white blood cells,which interferes with the production of normal blood cells.A therapeutic target that has been investigated in AML is cyciin-dependent kinase9（CDK9）,which an important regulator of transcriptional elongation,particularly for cancers driven by transcriptional ***,we developed compound HY009 that is extremely potent and highly selective against CDK9 with favorable oral pharmacokinetic *** found that HY-X-009 displaying a low nanomolar biochemical activity against CDK9 and an at least 200-fold selectivity against other *** of AML with HY-X-009 resulted in rapidly decreased of global p-Ser2 RNA polymerase Ⅱ levels and expression of the prosurvival protein Mcl-1,leading to rapid induction of apoptosis in vitro and in *** the in vivo studies HY-X-009 demonstrated a good bioavailability and significantly suppressed the tumor growth in MV4-11 cell inoculated xenograft model without exhibiting obvious ***,this study indicates that HY-X-009 showed strong potential as a novel treatment of AML.

关键词： AML CDK9 CDK9 inhibitor High selectivity

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Synthesis and biological evaluation of thalidomide derivatives as potential anti-psoriasis agents

Synthesis and biological evaluation of thalidomide derivativ...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Kaiwei Tang Chihhua Tseng School of Pharmacy College of PharmacyKaohsiung Medical University

A number of thalidomide derivatives were synthesized and evaluated for their anti-inflammatory *** of the benzyl group to the parent thalidomide is unfavorable in which2-(l-benzyl-2,6-dioxopiperidin-3-yl)isoindoline-l,3-dione(4 a) was ***,the inhibitory activities on TNF-α and IL-6 expression in HaCaT cells were improved by the substitution of chloro or methoxy group at the phenyl position of 4 *** IL-6 inhibitory activity decreased in an order of 5 c(69.44%) >4 c(48.73%) >6 c(3.19%) indicated 3-substituted derivative is more active than the 4-substituted counterpart which in turn is more active than the2-substituted counterpart Among them,2-[l-(3-chlorobenzyl)-2,6-dioxopiperidin-3-yl]isoindo line-1,3-dione(5 c) was found to inhibit TNF-a and IL-6 expression in HaCaT cells with a higher potency than thalidomide and no significant cell cytotoxicity was detected at 10μ*** psoriasis,Compound 5 c reduced IL-6,IL-8,IL-1β and IL-24 in both imiquimod-stimulated and TNF-α-stimulated *** results indicated that compound 5 c is a potential lead of novel anti-psoriasis *** optimization of compound 5 c and its in vivo assay are ongoing.

关键词： Thalidomide Psoriasis Tumor necrosis factor Anti-inflammatory Anti-proliferative

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Identification of TAK-632 and its analogs as potent inhibitors of necroptosis by targeting RIPK1 and RIPK3

Identification of TAK-632 and its analogs as potent inhibito...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Chunlin Zhuang Xiaofei Chen Zhenyuan Miao Zhenyu Cai Hongyang Wang Wannian Zhang School of Pharmacy Second Military Medical University The International Cooperation Laboratory on Signal Transduction Eastern Hepatobiliary Surgery HospitalSecond Military Medical University

Necroptosis is a form of programmed,caspase-independent cell death that is mediated by receptor-interacting protein kinases,RIPK1 and RIPK3,and the mixed lineage kinase domain-like(MLKL).Necroptosis contributes to the pathophysiology of various inflammatory,infectious and degenerative ***,identification of small molecule inhibitors for pathologic necroptosis has broad therapeutic *** this study,we identified that the pan-RAF kinase inhibitor TAK-632 is a potent inhibitor of necroptosis from an in-house fluorinated compound ***-632 inhibits RIPK1 and RIPK3 kinase activity and thus disrupted RIPK1-RIPK3 necrosome complex *** vivo,TAK-632 alleviates TNF-induced systemic inflammatory response syndrome(SIRS).A preliminary structure activity relationship(SAR) analysis of TAK-632 analogues were performed to generate a highly-potent,selective inhibitor for RIPK1/***,TAK-632 is an inhibitor of necroptosis and we could develop more selective and highly potent inhibitors for RIPK1/3 based on TAK-632 scaffold.

关键词： Necroptosis TAK-632 RIPK1 RIPK3 SAR

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Discovery of carbazole carboxamides as novel RORγt modulators

Discovery of carbazole carboxamides as novel RORγt modulato...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Yafei Huang Mingcheng Yu Chen Zhu Yurong Yan Huimin Guo Qiong,Xie Yonghui Wang Department of Medicinal Chemistry School of PharmacyFudan University

The retinoic acid receptor-related orphan receptor-gamma-t（RORγt） is a key nuclear receptor of the ROR family that has been implicated in the differentiation and function of Thl7 *** RORγt inverse agonists can be used as agents for inflammatory and autoimmune diseases,ROR t agonists can be developed as agents for cancer ***,we have reported the discovery of a series carbazole carboxamides as RORγt inverse *** SAR exploration,we found that after introducing a larger substituent at the6-position（2） or 9-position（3） on the carbazole ring of the carboxamide（1）,the function of the compound can be changed from an inverse agonist to a partial *** order to systematically explore the effect of different substitutions at these two positions on the activity and function of the compounds,we designed and synthesized some compounds with the 6-position（A-series） and 9-position（B-series） substituents changed from small to *** initial results from the RORγ dual FRET assay showed that when the substituents at 6-or9-position of the carbazole ring gradually increase,the function of the compounds appears to be gradually changed from inverse agonists to agonists to inverse *** this poster,we will present the design,synthesis and evaluation of carbazole carboxamide-based RORγt modulators.

关键词： RORγt modulators agonists inverse agonists carbazole carboxamides

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Privileged structure-derived design,synthesis and biological evaluation of novel DAPY analogues as potent HIV-1 NNRTIs

Privileged structure-derived design,synthesis and biological...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Ye Tian Dongwei Kang Zhaoqiang Liu Xiao Li Lingzi Zhang Boshi Huang Jun Wang Erik De Clercq Dirk Daelemans Christophe Pannecouque Peng Zhan Xinyong Liu Department of Medicinal Chemistry Key Laboratory of Chemical Biology(Ministry of Education)School of Pharmaceutical SciencesShandong University Rega Institute for Medical Research KU Leuven

Drug resistance and poor pharmacokinetic properties of the second generation of HIV-1 NNRTIs remains two main problems to be *** the present work,based on the crystal structure information,several privileged heterocyclic scaffolds were employed as the central core in the newly designed diarylpyrimidines（DAPY） ***,the cyanovinyl group as an optimized substituent in DAPY derivatives,was introduced in the left ***,five subseries of a total of 21 compounds were designed and *** results showed that 9 compounds exhibited single nanomolar EC values against WT HIV-1 *** them,YTB-17 a represents the best inhibitor with remarkable potencies against a panel of common clinical resistant mutants(EC values:L100 I = 11 nM,K103 N = 1.6 nM,E138 K = 2.8 nM,Y181 C = 29 nM,Y188 L = 160 nM,F227 L+V106 A = 84 nM).Further mouse liver microsomal stability study indicated the potential of YTB-17 a for detailed investigations.

关键词： HIV-1 NNRTIs DAPY privileged structure drug resistance drug design

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Application of new-type ASK1 inhibitor on treating hepatic fibrosis

Application of new-type ASK1 inhibitor on treating hepatic f...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Xiaomeng Zhang Chongxun Ge Liwen Zhao Nanjing Sanhome pharmaceutical Co.Ltd.

Apoptosis signal-regulating kinase 1（ASK1） is a major member of the mitogen-activated protein kinase（MAP3 Ks） group. When human body appeal signs of stress injuries and proinflammatory factors,ASKl will be induced and ***,the downstream JNK and p38-MAPK signaling pathway was activated which lead to regulate cell growing,differentiation,inflammation and apoptosis. Recent years,research on ASK1 inhibitors are found to have significant benefit on clinical practice on chronic hepatic diseases,such as non-alcoholic steatohepatitis（NASH） and hepatic *** have designed and synthesized several series of new *** optimization led to several more potent compounds than GS-4997,with an IC of 2-10 nM of ASK1 kinase inhibition,and an IC of 70-200 nM on LX-2 cell Coll1 A1 mRNA level in ***-PD assays indicated high bioavailability,tissue distribution and liver/plasma *** safety profile was achieved by testing in HL-7702 liver cell toxicity,hERG inhibition and Langendorff heart *** CCl-induced mice liver fibrosis model,reduced level of Coll1 A1 gene expression,hydroxyproline concentrations,hematoxylin-eosin staining was observed,without obvious loss in body weight These compounds are currently evaluated in further preclinical research to identify drug candidates.

关键词： ASK1 Hepatic Fibrosis Drug Discovery

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Chemically induced degradation of CK2 by a proteolysis targeting chimera based on ubiquitin-proteasome system

Chemically induced degradation of CK2 by a proteolysis targe...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Hong Chen Feihong Chen Shaohua Gou Pharmaceutical Research Center and School of Chemistry and Chemical Engineering Jiangsu Province Hi-Tech Key Laboratory for Biomedical ResearchSoutheast University

Although the development of targeted drugs has brought great advances to cancer treatments,most targeted drugs are limited to just inhibit the activity of protein with a high rate of *** targeting chimera（PROTAC） is a new strategy that utilizes a heterobifunctional compound to chemically induce the degradation of target protein by recruiting ubiquitin-proteasome system（UPS）. In our study,several PROTACs containing pomalidomide were designed and prepared via "click reaction" to degrade casein kinase 2（CK2） protein,a ubiquitous,highly pleiotropic and constitutively active serine/threonine protein kinase that is closely associated with tumorigenesis by its overexpression in cancer cells. One of our PROTACs was found to degrade CK2 in a dose and time-dependent manner,and keep CK2 at a low basal level by recruiting *** degradation of CK2 resulted in the reduced phosphorylation of Akt and the up-regulation of *** a CK2 protein degrader,the PROTAC also showed analogous cytotoxicity to CX-4945（a CK2 inhibitor） toward CK2 overexpressed cancer cells like MDA-MB-231,but with a quite different mechanism of *** of CK2 overexpression in most tumors,PROTAC targeting CK2 degradation can be a potential way for cancer treatment

关键词： casein kinase 2 protein degradation proteolysis targeting chimeras CX-4945 pomalidomide

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Studies on molecular design,biological activity and action mechanism of histidine-rich β-hairpin peptides

Studies on molecular design,biological activity and action m...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Chensi Wang Chenyu Xue Xinran Li Xinyao Xu Na Dong Animal Science and Technology Collage Northeast Agricultural University

The increasing appearance of multidrug-resistant pathogens has created an urgent need for desirable suitable alternatives to current *** peptides（AMPs）,which act as defensive weapons against microbes,have received great attention because of broad-spectrum activities,unique antibiotic-resistant ***,the interaction of structure and function remain indistinct,especially,there is a lack of a definitive and regular template to design a new antimicrobial *** the present study,the engineered peptides were based on histidine（His,H） according to the following sequence template RR（XH）nXPGX（HX）nRR（n=1,2,3）,and the relationship between strand length and biological activities was *** results showed that the peptides exhibit more beta-hairpin structure in a lipid environment that mimics cell *** addition,the symmetric terminal antimicrobial peptide HV2 rich in His with the β-hairpin structure displayed a strong antibacterial activity against Gram-negative strains and almost no toxicity and hemolytic activity to normal ***2 decreased hemolytic activity 64 times than *** results of the antibacterial mechanism showed that the antimicrobial peptide HV2 acted on the bacterial cell membrane and increased their permeability,resulting in cell membrane disruption and *** the LPS inflammation model test,it was found that HV2 had a better anti-inflammatory effect at 32 μ*** summary,HV2 exhibits high bactericidal activity and cell selectivity,making it a promising candidate for future antibiotics.

关键词： β-Hairpin antimicrobial peptides Histidine Biological activity Bactericidal mechanism

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Optimization of N2,N4-disubstituted quinazoline-2,4-diamines with improved potency against K103 N mutant and rilpivirine-resistant E138K mutant as novel HIV-1 non-nucleoside reverse transcriptase inhibitors

Optimization of N2,N4-disubstituted quinazoline-2,4-diamines...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Sheng Han Erik De Clercq Christophe Pannecouque Ge Meng Fener Chen Engineering Center of Catalysis and Synthesis for Chiral Molecules Department of ChemistryFudan University Shanghai Engineering Center of Industrial Asymmetric Catalysis for Chiral Drugs Rega Institute for Medical Research KU Leuven

A series of N2,N4-disubstituted quinazoline-2,4-diamines derivatives as the new HIV-1 non-nucleoside reverse transcriptase inhibitors（NNRTIs） was designed and synthesized in this paper（Figure 1）.Most of these compounds showed potent inhibition of the HIV-1 WT strain and the mutant strain K103 N,Y181 C,E138 K with low nanomolar EC50 *** most potent compound H-29 displayed an EC value of 3.6 nM against HIV-1 ⅢB,3.3 nM against K103 N,2.8 nM against E138 K among all the tested *** also showed the better potency against the drug-resistant mutant strain E138 K than the FDA approved drugs ***,H-29 showed the higher selectively index（SI） value than that of rilpivirine（Figure 1）.

关键词： DAPY HIV NNRTI quinazoline SARs

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Synthesis of GAGs natural products and mimetics based on semi-synthetic strategy and the discovery of hit compounds

Synthesis of GAGs natural products and mimetics based on sem...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Zhongjun Li Wang Yao Xiao Zhang Huiying Liu Mingyi Wu State Key Laboratory of Natural and Biomimetic Drugs Department of Chemical BiologySchool of Pharmaceutical SciencesPeking University State Key Laboratory of Phytochemistry and Plant Resources in West China Kunming Institute of BotanyChinese Academy of Sciences

Glycosaminoglycans(GAGs) as one major part of the glycocalyx are involved in many essential biological cell *** for hyaluronic acid,other GAGs(such as chondroitin sulfate,heparin,etc.) are linked to proteins and exist as *** and more attention has been attracted to GAGs because of their potential therapeutic ***,further biological studies and medicinal researches have been hindered by the scarcity of homogeneous *** order to obtain well-defined GAG oligosaccharides and reduce cumbersome protecting group modification and iterative glycosylations,our group has developed a semi-synthetic strategy by enzymatic or acidic degradation of commercial hyaluronic acid or chondroitin sulfate,which can afford structurally defined GAG *** simple protecting group manipulations or glycosylation modification,natural GAG oligosaccharides can be obtained,and the structure derivatization can be performed *** have shown that sulfated hyaluronic acid oligosaccharides(sHA) can promote the growth of axons,and the sulfation pattern significantly affects its *** chondroitin sulfate oligosaccharides(FuCS) exhibit excellent anticoagulant activity with reduced risks of adverse effects and *** strategy provides a concise synthesis method for GAG oligosaccharides and their mimics,which is of great significance for promoting the medicinal chemistry research of GAGs.

关键词： chondroitin sulfate hyaluronic acid semi-synthesis drug discovery

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