Jyothi Damodara, Sheetal Tresa Fernandes, Smitha Maria DSouza
{"title":"Evaluation of 1,3-Thiazole Derivatives with Pharmaceutical and Chemical Activity: a Review","authors":"Jyothi Damodara, Sheetal Tresa Fernandes, Smitha Maria DSouza","doi":"10.3987/rev-23-1003","DOIUrl":"https://doi.org/10.3987/rev-23-1003","url":null,"abstract":"","PeriodicalId":13166,"journal":{"name":"Heterocycles","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"70752119","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Chandi C. Malakar, K. Kant, Sourav Banerjee, Chandresh K. Patel, S. Kalita, N. Aljaar, Reetu Reetu, Priyadarshini Naik
{"title":"Advances on Catalytic Approaches towards the Synthesis of Quinoline Derivatives Using Povarov Reaction","authors":"Chandi C. Malakar, K. Kant, Sourav Banerjee, Chandresh K. Patel, S. Kalita, N. Aljaar, Reetu Reetu, Priyadarshini Naik","doi":"10.3987/rev-23-1004","DOIUrl":"https://doi.org/10.3987/rev-23-1004","url":null,"abstract":"","PeriodicalId":13166,"journal":{"name":"Heterocycles","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"70752286","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Hai Xie, Lei Zhang, Xiu-Ting Qin, Ji Li, Ya-Li Zhang, Jin-Yu Li
{"title":"A Convenient Synthesis of 1,2,4-Triazino[2,3-b]indazol-3-amine Derivatives via Tandem Abnormal Staudinger/Aza-Wittig/Isomerization Reaction","authors":"Hai Xie, Lei Zhang, Xiu-Ting Qin, Ji Li, Ya-Li Zhang, Jin-Yu Li","doi":"10.3987/com-23-14889","DOIUrl":"https://doi.org/10.3987/com-23-14889","url":null,"abstract":"","PeriodicalId":13166,"journal":{"name":"Heterocycles","volume":"42 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135445254","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Dongdong Guo, Jiang Geng, Jinyi Shi, Jin Wang, Jiaxian Li, Lin Jiao
{"title":"Simple Brønsted Acid Catalyzed Three-Component Reactions for Efficient Alkylation of Indolizines with Aromatic Aldehydes and Hantzsch Esters","authors":"Dongdong Guo, Jiang Geng, Jinyi Shi, Jin Wang, Jiaxian Li, Lin Jiao","doi":"10.3987/com-23-14898","DOIUrl":"https://doi.org/10.3987/com-23-14898","url":null,"abstract":"","PeriodicalId":13166,"journal":{"name":"Heterocycles","volume":"73 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135508714","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"A Review on Indole[2,3-a]quinolizidine: The Synthetic Approaches to the Development of Bioactive Indolo[2,3-a]quinolizidine Scaffolds","authors":"Shivendra Singh, Yukti Monga, Shivangi Sharma, Ashu Gupta","doi":"10.3987/rev-23-1008","DOIUrl":"https://doi.org/10.3987/rev-23-1008","url":null,"abstract":"","PeriodicalId":13166,"journal":{"name":"Heterocycles","volume":"15 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136004420","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
H. Akber Aisa, C. Niu, Heng Wu, Ayitila Maimaitijiang, Dan-Jie Tang, Baoxing Xie
– Based on non-classical bioisosterism and the rule of alkene insertion, thirty-five heterocyclic aurones and its analogue indanones derivatives were designed and synthesized. They were evaluated for inhibitory activity against HELA, HT-29 and A549 and HepG2 human cancer cell lines. Among them, twenty-five compounds exhibited moderate to excellent antitumor activity. The minimum value of IC 50 was 1.649±0.083 μM (compound B1 ). The SAR showed that aurone with B ring as aromatic heterocycles such as 4-bromothiophene, quinoline, carbazole and indanone derivatives and some or indanone were more potent than others. Besides, the introduction of acetylated glycosides was beneficial to the activity. Compounds A1 , B1 , C5 , C8 , C10 , C11 , C12 and D1 were promising antitumor agents. Among them, compounds molecular docking studies were performed between B1 , C8 and potential targets Aurora B (PBD: 2BFY). On the basis, the chemical and physical properties, as well as ADMET of active compounds were predicted and analyzed. And it showed that most of compounds had good pharmacokinetic profiles and high safety profiles
-基于非经典生物等构和烯烃插入规律，设计合成了35个杂环金酮及其类似物吲哚酮衍生物。测定了它们对HELA、HT-29、A549和HepG2人癌细胞的抑制活性。其中25个化合物具有中等至优异的抗肿瘤活性。IC 50最小值为1.649±0.083 μM(化合物B1)。SAR结果表明，4-溴噻吩、喹啉、咔唑和吲哚酮衍生物等含B环的芳香杂环的呋喃酮具有较强的药效。此外，乙酰化糖苷的引入有利于活性的提高。化合物A1、B1、C5、C8、C10、C11、C12和D1是有前景的抗肿瘤药物。其中，化合物B1、C8与潜在靶点Aurora B (PBD: 2BFY)进行了分子对接研究。在此基础上，对活性化合物的理化性质和ADMET进行了预测和分析。结果表明，大多数化合物具有良好的药动学特征和较高的安全性
{"title":"Synthesis and Antitumor Activity of Heterocylic Aurone and Its Analogue Indanone Derivatives","authors":"H. Akber Aisa, C. Niu, Heng Wu, Ayitila Maimaitijiang, Dan-Jie Tang, Baoxing Xie","doi":"10.3987/com-22-14764","DOIUrl":"https://doi.org/10.3987/com-22-14764","url":null,"abstract":"– Based on non-classical bioisosterism and the rule of alkene insertion, thirty-five heterocyclic aurones and its analogue indanones derivatives were designed and synthesized. They were evaluated for inhibitory activity against HELA, HT-29 and A549 and HepG2 human cancer cell lines. Among them, twenty-five compounds exhibited moderate to excellent antitumor activity. The minimum value of IC 50 was 1.649±0.083 μM (compound B1 ). The SAR showed that aurone with B ring as aromatic heterocycles such as 4-bromothiophene, quinoline, carbazole and indanone derivatives and some or indanone were more potent than others. Besides, the introduction of acetylated glycosides was beneficial to the activity. Compounds A1 , B1 , C5 , C8 , C10 , C11 , C12 and D1 were promising antitumor agents. Among them, compounds molecular docking studies were performed between B1 , C8 and potential targets Aurora B (PBD: 2BFY). On the basis, the chemical and physical properties, as well as ADMET of active compounds were predicted and analyzed. And it showed that most of compounds had good pharmacokinetic profiles and high safety profiles","PeriodicalId":13166,"journal":{"name":"Heterocycles","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"70398643","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Qianjun Zhang, Lin Zhang, Jun Zheng, Xuan Wang, Z. Tao
{"title":"Supramolecular Self-Assembly Based on Symmetric Tetramethyl-Substituted Cucurbit[6]uril and Small Aromatic Amines","authors":"Qianjun Zhang, Lin Zhang, Jun Zheng, Xuan Wang, Z. Tao","doi":"10.3987/com-22-14771","DOIUrl":"https://doi.org/10.3987/com-22-14771","url":null,"abstract":"","PeriodicalId":13166,"journal":{"name":"Heterocycles","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"70398819","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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