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Discovery of Novel Tricyclic 5H-Pyridazino[4,5-b]indoles as Potent Antitumor Agents： Design, Synthesis and Biological Evaluation

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Chemical Research in Chinese Universities 2015年第3期31卷 372-380页

作者： zhai xin WANG Limei SHI Jiyue GONG Ping Key Laboratory of Structure-based Drug Design and Discovery Ministry of EducationShenyang Pharmaceutical University Shenyang 110016 P.R.China

A novel series of 5H-pyridazino[4,5-b]indoles（L-01-L-32） was synthesized and characterized by means of 1H NMR, MS and elemental analysis. The cytotoxicity of the target compounds against Bel-7402 and HT-1080 cell lines were evaluated by 3-（4,5-dimethylthiazol-2-y1）-2,5-diphenyltetrazolium bromide（MTT） assay. Most of them exhibited moderate to excellent cytotoxicity, and six compounds（L-04, L-06, L-18, L-20, L-21 and L-23） possessed dramatically increased cytotoxicity superior to Gefitinib. Of these initial hits, compound L-21 displayed remarkable cytotoxicity against the tested cell lines with half maximal inhibitory concentration（IC50） values of 4.6 and 2.1 μmol/L, respectively, which was 13.9- to 25.6-fold more potent than positive control.

关键词： 1-Anilino-5H-pyridazino[4,5-b]indole EGFR inhibitor Cytotoxicity

Syntheses and Antiproliferative Activities of Novel Diarylthiosemicarbazide Derivatives

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Chemical Research in Chinese Universities 2013年第1期29卷 62-66页

作者： zhai xin HE Ying YANG Zhen GONG Ping Key Laboratory of Structure-Based Drug Design & Discovery Ministry of Education School of Pharmaceutical Engineering Shenyang Pharmaceutical University Shenyang 110016 P. R. China

A series of novel N-methylpicolinamide-moiety containing diarylthiosemicarbazide derivatives was prepared and evaluated for their in vitro antiproliferative activity against three cancer cell lines（human alveolar epithelial cell A549, human lung cancer cell H460 and human colorectal cancer cell HT-29） by 3-（4,5-dimethyl）thiazolyldiphenyltetrazoliumromide（MTT） assay. Six compounds（Tb--7g） with halogen substituents exhibited preferable cytotoxicity against one or more cell lines in a low micromolar range. Especially, the most promising compound 7g exhibited remarkable antiproliferative activity with the IC50 values of 2.2, 1.8 and 5.2 μmol/L against A549, H460 and HT-29 cell lines respectively, which is comparable to sorafenib.

关键词： Thiosemicarbazide N-methylpicolinamide Antiproliferative activity

Synthesis and Antibacterial Activity of Novel Oxazolidinone Analogs Containing Substituted Thiazole/Fused-Bicyclic Groups

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Chemical Research in Chinese Universities 2006年第4期22卷 459-464页

作者： zhai xin ZHAO Yan-fang WANG Jia HONG Wei HUANG Liang GONG Ping School of Pharmaceutical Engineering Shenyang Pharmaceutical University Shenyang 110016 P. R. China

Sixteen novel oxazolidinone analogs containing substituted thiazole/fused-bicyclic（imidazo[ 1,2-b] pyridazine/ imidazo[2,1-b] thiazole） groups were designed and synthesized. A new method for the preparation of the key intermediate compound 11 was proposed. The structures of the target compounds were confirmed by ^1H NMR, IR and MS, and their in vitro antibacterial activities against staphylococcus aureus were evaluated. Among them, compound 16a displays a promising antibacterial activity comparable to that of linezolid.

关键词： Oxazolidinone analog Synthesis Antibacterial activity

Syntheses and Vasodilatory Activities of New Pyrazolo[4,3-d]pyrimidin-7-ones

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Chemical Research in Chinese Universities 2006年第4期22卷 468-473页

作者： ZHAO Yan-fang zhai xin CHEN Jiao-yue GUO Shu-chun GONG Ping School of Pharmaceutical Engineering Shenyang Pharmaceutical University Shenyang 110016 P.R. China

A series of novel pyrazolo [ 4,3-d ] pyrimidin-7-ones was designed and synthesized in order to find new potent phosphodiesterase 5 inhibitors（PDE5）. The structures of all the compounds were confirmed by IR, ^1H NMR and MS; their in vitro vasodilatory activities were tested on isolated rabbit aortic spiral strips. Among them, compound X3 displays a significant vasodilatory activity, which is more potent than verapamil.

关键词： Pyrazolo[4,3-d]pyrimidin-7-one Synthesis Vasodilatory activity

Design,synthesis and antiproliferative activities of novel 5H-pyridazino[4,5-b]indoles

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Chinese Chemical Letters 2007年第10期18卷 1191-1194页

作者： Rong Dong Li xin zhai Yan Fang Zhao Ping Gong School of Pharmaceutical Engineering Shenyang Pharmaceutical University Shenyang 110016 China School of Pharmacy Hunan University of Traditional Chinese Medicine Changsha 410208 China

A novel series of 5H-pyridazino[4,5-b]indoles were designed and synthesized in order to find novel potent anticancer compounds. The structures were confirmed by ^1H NMR and MS. Their antiproliferative activities against two cancer cell lines were tested by the MTT method in vitro. Three of compounds （1e, 1g, and 1h） exhibited potent antiproliferative activities, especially compound lh （with IC50 values of 5.2 μmol/L and 1.9 μmol/L against Bel-7402 and HT-1080, respectively）. The preliminary structure-activity relationships of 5H-pyridazino[4,5-b]indole derivatives were discussed.

关键词： 5H-pyridazino[4,5-b]indole derivatives Synthesis Antiproliferative activities

Design,synthesis and antiproliferative activity of novel 2,7-disubstituted triazolo[1,5-a]pyrimidines

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Chinese Chemical Letters 2009年第10期20卷 1179-1182页

作者： xin zhai Nan Jiang Ke Liang Zhang Feng Bao Ping Gong Key Lab of New Drugs Design and Discovery of Liaoning Province School of Pharmaceutical Engineering Shenyang Pharmaceutical University Shenyang 110016 China Liaoning Food and Drug Administration Technical Evaluation Center Shenyang 110003 China

In our efforts to identify novel potent anticancer agents, we synthesized a series of 2,7-disubstituted triazolo[1,5-a]pyrimidines （6-16）. Their antiproliferative activity against Bel-7402, HT- 1080 and WI-38 cell lines was tested by MTT assay in vitro. Four of the compounds （9-11 and 16） displayed promising antiproliferative activity superior to gefitinib, especially compound 9. A preliminary SAR study of these derivatives was performed.

关键词： Triazolo[1,5-a]pyrimidines Synthesis Antiproliferative activity

Chemical renal artery denervation with appropriate phenol in spontaneously hypertensive rats

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Journal of Geriatric Cardiology 2018年第11期15卷 695-702页

作者： Ming WANG Wen-Zheng HAN Min ZHANG Wei-Yi FANG xin-Rong zhai Shao-Feng GUAN xin-Kai QU Department of Cardiology Huadong Hospital Affiliated to Fudan University Shanghai China Shanghai Key Laboratory of Clinical Geriatric Medicine Shanghai China Department of Cardiology Shanghai Chest Hospital Shanghai Jiaotong University Shanghai China

Objective To explore the effectiveness of renal denervation (RDN) on blood pressure with the appropriate dosage of phenol/ethanol solution in spontaneously hypertensive rats (SHRs). Methods RDN was performed on the bilateral renal artery. Forty SHRs were divided into four groups according on the dosage of phenol (10% phenol in absolute ethanol): sham group, 0.5 mL phenol group, 1 mL phenol group and 1.5 mL phenol group (n = 10 in each group). Blood pressure was measured by tail-cuff plethysmography. Plasma creatinine was determined four weeks after the treatment. The kidneys and renal arteries were collected and processed for histological examination. Results A sustained decrease in systolic blood pressure (SBP) was only observed after the application of 1 mL phenol for four weeks, while SBP was lowered during the first week after RDN and increased in the following three weeks in the 0.5 mL and 1.5 mL phenol groups compared with the sham group. Renal norepinephrine (NE) was significantly decreased four weeks after RDN in the 1 mL and 1.5 mL phenol group compared with the sham group, but not in the 0.5 ml group. RDN with 1 mL phenol obviously reduced glomerular fibrosis. Histopathological analysis showed that tyrosine hydroxylase immunoreactivity was lower in the 1 mL and 1.5 mL phenol groups compared with the sham group. Moderate renal artery damage occurred in the 1.5 mL phenol group. Conclusion Chemical denervation with 1 ml phenol (10% phenol in absolute ethanol) effectively and safely damaged peripheral renal sympathetic nerves and contributed to the sustained reduction of blood pressure in SHRs.

关键词： Hypertension Norepinephrine Phenol Renal denervation Spontaneously hypertensive rats

Synthesis and in vitro cytotoxicity of novel 1,4-disubstituted phthalazines

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Chinese Chemical Letters 2008年第1期19卷 29-32页

作者： xin zhai Juan Li Lei He Su Zheng Yao Bin Zhang Ping Gong School of Pharmaceutical Engineering Shenyang Pharmaceutical University Shenyang 110016 China Shenyang No. 1 Pharmaceutical Factory Northeast Pharmaceutical Group Co. Ltd. Shenyang 110023 China

Eight novel 1,4-disubstituted phthalazines （7-14） were designed and synthesized. The structures of all the synthesized compounds were confirmed by IR,1H NMR, 13C NMR, MS and elemental analysis. Their in vitro cytotoxicity against cancer cell lines （Bel-7402 and HT- 1080） were evaluated by standard MTT assay. Among them, compounds 9 and 11 exhibited more potent cytotoxicity than cisplatin. 2007 Ping Gong. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.

关键词： Phthalazine derivatives Synthesis Cytotoxicity

Synthesis and cytotoxicity studies of quinoline-3-carbonitrile derivatives

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Chinese Chemical Letters 2010年第8期21卷 939-942页

作者： Shu Lan Zhang xin zhai Shi Jiao Zhang Hong Hao Yu Ping Gong Key Laboratary of Original New Drugs Design and Discovery of Ministry of Education School of Pharmaceutical Engineering Shenyang Pharmaceutical UniversityShenyang 110016China

A series of quinoline-3-carbonitrile derivatives were designed and *** cytotoxicity in vitro against four cancer cell lines（A549,HT-29,MDA-MB-231 and SMMC-7721） were evaluated by standard MTT *** pharmacological results showed that most of the prepared compounds displayed excellent selective cytotoxicity toward SMMC-7721 cell *** them, compounds 7c,7e,11b,11f and 11g were more active than Gefitinb against SMMC-7721 cell line.

关键词： Quinoline-3-carbonitrile Synthesis Cytotoxicity