Pub Date : 2020-03-03DOI: 10.1080/10426507.2019.1672691
S. Matavos-Aramyan, Sadaf Soukhakian, M. Jazebizadeh
Abstract A large variety of organosulfur compounds has been shown to exhibit diverse biological effects such as anti-oxidant effects, anti-inflammatory properties, inhibition of platelet aggregation, reduction of systolic blood pressure, and reduction of cholesterol. In addition, these sulfoxides and sulfones show wide and significant applications as commodity chemicals in various fields of chemistry. Thus, the synthesis of sulfoxides and sulfones has remained a point of attraction for synthetic organic chemists. Selected from an array of methods used to synthesize the sulfoxides or sulfones, oxidation of sulfides is the most promising one. This review summarizes chemoselective methods for the synthesis of the sulfoxides and sulfones with focus on the oxidative protocols, which will help researchers to explore and utilize the mentioned protocols for different organic transformations. Graphical Abstract
{"title":"Selected methods for the synthesis of sulfoxides and sulfones with emphasis on oxidative protocols","authors":"S. Matavos-Aramyan, Sadaf Soukhakian, M. Jazebizadeh","doi":"10.1080/10426507.2019.1672691","DOIUrl":"https://doi.org/10.1080/10426507.2019.1672691","url":null,"abstract":"Abstract A large variety of organosulfur compounds has been shown to exhibit diverse biological effects such as anti-oxidant effects, anti-inflammatory properties, inhibition of platelet aggregation, reduction of systolic blood pressure, and reduction of cholesterol. In addition, these sulfoxides and sulfones show wide and significant applications as commodity chemicals in various fields of chemistry. Thus, the synthesis of sulfoxides and sulfones has remained a point of attraction for synthetic organic chemists. Selected from an array of methods used to synthesize the sulfoxides or sulfones, oxidation of sulfides is the most promising one. This review summarizes chemoselective methods for the synthesis of the sulfoxides and sulfones with focus on the oxidative protocols, which will help researchers to explore and utilize the mentioned protocols for different organic transformations. Graphical Abstract","PeriodicalId":20043,"journal":{"name":"Phosphorus Sulfur and Silicon and The Related Elements","volume":"95 1","pages":"181 - 193"},"PeriodicalIF":0.0,"publicationDate":"2020-03-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79174769","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-03-03DOI: 10.1080/10426507.2019.1673749
I. Nizamov, R. Salikhov, I. D. Timushev, Yevgeniy N. Nikitin, I. Nizamov, V. Y. Yakimov, M. Shulaeva, O. K. Pozdeev, E. S. Batyeva, R. Cherkasov, A. S. Ponomareva
Abstract A new series of chiral carboxypyridinium dithiophosphates were synthesized by the reactions of nicotinic, isonicotinic, and picolinic acids with dithiophosphoric acid on the basis (1S)-endo-(–)-borneol in benzene or ethanol. 5,5-Dimethyl-2-mercapto-2-thiono-1,3,2-dioxaphosphorinane reacted with 3-hydroxypyridine or 3-pyridinemethanol in EtOH to afford the 3-hydroxypyridinium and 3-hydroxymethylpyridinium 5,5-dimethyl-2-mercapto-2-thiono-1,3,2-dioxaphosphorinanes which possessed antifungal activity against Candida albicans. Graphical Abstract
{"title":"Pyridinium salts of dithiophosphoric acids on the basis of nicotinic acids and their isomers, 3-hydroxypyridine, and 3-pyridinemethanol","authors":"I. Nizamov, R. Salikhov, I. D. Timushev, Yevgeniy N. Nikitin, I. Nizamov, V. Y. Yakimov, M. Shulaeva, O. K. Pozdeev, E. S. Batyeva, R. Cherkasov, A. S. Ponomareva","doi":"10.1080/10426507.2019.1673749","DOIUrl":"https://doi.org/10.1080/10426507.2019.1673749","url":null,"abstract":"Abstract A new series of chiral carboxypyridinium dithiophosphates were synthesized by the reactions of nicotinic, isonicotinic, and picolinic acids with dithiophosphoric acid on the basis (1S)-endo-(–)-borneol in benzene or ethanol. 5,5-Dimethyl-2-mercapto-2-thiono-1,3,2-dioxaphosphorinane reacted with 3-hydroxypyridine or 3-pyridinemethanol in EtOH to afford the 3-hydroxypyridinium and 3-hydroxymethylpyridinium 5,5-dimethyl-2-mercapto-2-thiono-1,3,2-dioxaphosphorinanes which possessed antifungal activity against Candida albicans. Graphical Abstract","PeriodicalId":20043,"journal":{"name":"Phosphorus Sulfur and Silicon and The Related Elements","volume":"80 1","pages":"226 - 230"},"PeriodicalIF":0.0,"publicationDate":"2020-03-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76007380","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Abstract A one-pot synthetic strategy was developed for the synthesis of heterocyclic 1,4,2-oxazaphosphinanes via a three component Kabachnik-Fields reaction of 2-aminophenol, diphenyl H-phosphonate and carbonyl compounds. Through this newly developed method, 12 organophosphorus heterocycles and 2 related chrysin derivatives were synthesized with high yields. The target compounds were characterized by 1H, 31P and 13C NMR and MS. Graphical Abstract
{"title":"Synthesis of 2-phenoxyl-2-oxo-1,4,2-oxazaphosphinanes from a three component reaction","authors":"Wen-jie Zhang, Xiling Ding, Zi-Jie Li, Wenzhu Bi, Xiaolan Chen, Yufen Zhao","doi":"10.1080/10426507.2019.1700417","DOIUrl":"https://doi.org/10.1080/10426507.2019.1700417","url":null,"abstract":"Abstract A one-pot synthetic strategy was developed for the synthesis of heterocyclic 1,4,2-oxazaphosphinanes via a three component Kabachnik-Fields reaction of 2-aminophenol, diphenyl H-phosphonate and carbonyl compounds. Through this newly developed method, 12 organophosphorus heterocycles and 2 related chrysin derivatives were synthesized with high yields. The target compounds were characterized by 1H, 31P and 13C NMR and MS. Graphical Abstract","PeriodicalId":20043,"journal":{"name":"Phosphorus Sulfur and Silicon and The Related Elements","volume":"16 1","pages":"359 - 366"},"PeriodicalIF":0.0,"publicationDate":"2020-02-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88792211","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-01-02DOI: 10.1080/10426507.2019.1688919
M. Rudd
Recently, I received a correspondence from Professor Andrey Karasik, Head of the A.E. Arbuzov Institute of Organic and Physical Chemistry in Tatarstan, Russia, and Member of the Awarding Committee for the International Arbuzovs Prize in Organophosphorus Chemistry. The International Arbuzovs Prize in the Field of Organophosphorus Chemistry was established in memory of the outstanding Russian chemists, Alexander and Boris Arbuzovs, by the President of the Republic of Tatarstan in 1997. The Arbuzovs Prize is awarded biennially to an honored Russian or foreign chemist for a “single scientific achievement or a set of scientific results in the development of phosphorus chemistry.” Professor Karasik wrote: “Laureates of the International Arbuzovs Prize are outstanding scientists from the leading scientific centers of the USA, Japan, China and Europe.” Past winners of the award include: 1997 – Professors Arkady Pudovik (Russia) and Louis Quin (USA) 1999 – Professor Jan Michalski (Poland) 2001 – Professor Francois Mathey (France) 2003 – Professor Edgar Niecke (Germany) 2005 – Professor Masaaki Yoshifuji (Japan) 2007 – Professor Irina P. Beletskaya (Russia)† 2009 – Professor Marian Mikolajczyk (Poland) 2011 – Professor Michael Blackburn (United Kingdom) 2013 – Professor Valerii Kukhar (Ukraine) 2015 – Professor Yufen Zhao (China) 2017 – Professor Manfred Scheer (Germany) ( indicates Editorial/Emeritus Board Member of Phosphorus Sulfur and Silicon and the Related Elements) For 2019, the international committee has chosen Professor Oleg Sinyashin as the winner of this prestigious prize. The presentation of the medal and diploma was made at the Academy of Sciences of the Republic of Tatarstan on 21 October 2019. The Prime Minister of the Republic of Tatarstan bestowed this honor at a ceremony that included many public officials and members of the scientific community, and was followed by a lecture by Professor Sinyashin entitled “Phosphorus as a Structure Forming Element in Organic and Inorganic Chemistry.” The citation indicates that the Awarding Committee recognizes [his] “fundamental results in the synthesis structure and reactivity of trivalent phosphorus compounds and their application in coordination and organometallic chemistry as well as for developing new scientific direction – selective electrochemical activation and functionalization of organic molecules and elemental (white) phosphorus.” He follows Professor Pudovik as the second winner of the Arbuzovs Prize from the School of Chemistry in Kazan.
最近，我收到了俄罗斯鞑靼斯坦A.E.阿尔布佐夫有机和物理化学研究所所长、国际阿尔布佐夫有机磷化学奖颁奖委员会成员安德烈·卡拉西克教授的来信。1997年，鞑靼斯坦共和国总统为纪念杰出的俄罗斯化学家亚历山大·阿尔布佐夫和鲍里斯·阿尔布佐夫而设立了国际有机磷化学奖。阿尔布佐夫奖每两年颁发一次，以表彰俄罗斯或外国化学家“在磷化学发展方面取得的一项或一系列科学成果”。卡拉西克教授写道:“国际阿布佐夫奖的获奖者是来自美国、日本、中国和欧洲主要科学中心的杰出科学家。”该奖项的往届获奖者包括:1997 - Arkady Pudovik教授(俄罗斯)和Louis Quin教授(美国)1999 - Jan Michalski教授(波兰)2001 - Francois Mathey教授(法国)2003 - Edgar Niecke教授(德国)2005 - Yoshifuji Masaaki教授(日本)2007 - Irina P. Beletskaya教授(俄罗斯)†2009 - Marian Mikolajczyk教授(波兰)2011 - Michael Blackburn教授(英国)2013 - Valerii Kukhar教授(乌克兰)2015 -赵玉芬教授(中国)2017 - Manfred Scheer教授(德国)((《磷、硫、硅及相关元素》编辑/名誉委员会成员)2019年，国际委员会选择奥列格·辛雅辛教授为这一著名奖项的获得者。奖章和文凭于2019年10月21日在鞑靼斯坦共和国科学院颁发。鞑靼斯坦共和国总理在包括许多政府官员和科学界成员在内的仪式上授予了这一荣誉，随后Sinyashin教授发表了题为“磷作为有机和无机化学中的结构形成元素”的演讲。颁奖词表明，评委会认可他“在三价磷化合物的合成结构和反应性方面取得的基础性成果，及其在配位和有机金属化学中的应用，以及在有机分子和单质(白磷)的选择性电化学活化和功能化方面开辟了新的科学方向。”他是继Pudovik教授之后，第二个来自喀山化学学院的Arbuzovs奖得主。
{"title":"Award announcement: Laureate of the International Arbuzovs Prize in organophosphorus chemistry for 2019","authors":"M. Rudd","doi":"10.1080/10426507.2019.1688919","DOIUrl":"https://doi.org/10.1080/10426507.2019.1688919","url":null,"abstract":"Recently, I received a correspondence from Professor Andrey Karasik, Head of the A.E. Arbuzov Institute of Organic and Physical Chemistry in Tatarstan, Russia, and Member of the Awarding Committee for the International Arbuzovs Prize in Organophosphorus Chemistry. The International Arbuzovs Prize in the Field of Organophosphorus Chemistry was established in memory of the outstanding Russian chemists, Alexander and Boris Arbuzovs, by the President of the Republic of Tatarstan in 1997. The Arbuzovs Prize is awarded biennially to an honored Russian or foreign chemist for a “single scientific achievement or a set of scientific results in the development of phosphorus chemistry.” Professor Karasik wrote: “Laureates of the International Arbuzovs Prize are outstanding scientists from the leading scientific centers of the USA, Japan, China and Europe.” Past winners of the award include: 1997 – Professors Arkady Pudovik (Russia) and Louis Quin (USA) 1999 – Professor Jan Michalski (Poland) 2001 – Professor Francois Mathey (France) 2003 – Professor Edgar Niecke (Germany) 2005 – Professor Masaaki Yoshifuji (Japan) 2007 – Professor Irina P. Beletskaya (Russia)† 2009 – Professor Marian Mikolajczyk (Poland) 2011 – Professor Michael Blackburn (United Kingdom) 2013 – Professor Valerii Kukhar (Ukraine) 2015 – Professor Yufen Zhao (China) 2017 – Professor Manfred Scheer (Germany) ( indicates Editorial/Emeritus Board Member of Phosphorus Sulfur and Silicon and the Related Elements) For 2019, the international committee has chosen Professor Oleg Sinyashin as the winner of this prestigious prize. The presentation of the medal and diploma was made at the Academy of Sciences of the Republic of Tatarstan on 21 October 2019. The Prime Minister of the Republic of Tatarstan bestowed this honor at a ceremony that included many public officials and members of the scientific community, and was followed by a lecture by Professor Sinyashin entitled “Phosphorus as a Structure Forming Element in Organic and Inorganic Chemistry.” The citation indicates that the Awarding Committee recognizes [his] “fundamental results in the synthesis structure and reactivity of trivalent phosphorus compounds and their application in coordination and organometallic chemistry as well as for developing new scientific direction – selective electrochemical activation and functionalization of organic molecules and elemental (white) phosphorus.” He follows Professor Pudovik as the second winner of the Arbuzovs Prize from the School of Chemistry in Kazan.","PeriodicalId":20043,"journal":{"name":"Phosphorus Sulfur and Silicon and The Related Elements","volume":"24 1","pages":"1 - 2"},"PeriodicalIF":0.0,"publicationDate":"2020-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76339445","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-10-03DOI: 10.1080/10426507.2019.1665235
{"title":"Foreword for international conference on phosphorus, boron and silicon 2018","authors":"","doi":"10.1080/10426507.2019.1665235","DOIUrl":"https://doi.org/10.1080/10426507.2019.1665235","url":null,"abstract":"","PeriodicalId":20043,"journal":{"name":"Phosphorus Sulfur and Silicon and The Related Elements","volume":"32 1","pages":"947 - 947"},"PeriodicalIF":0.0,"publicationDate":"2019-10-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73972155","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-08DOI: 10.1080/10426507.2019.1633316
Bao-Qiang Zhang, Lanxiang Shi
Abstract In a one-pot procedure, CuBr2 has been used as a efficient desulfurizing agent in the synthesis of 2-aminothiazoles by the condensation of in situ-generated 1-substituted thioureas from their dithiocarbamic acid salts, with in situ-generated α-bromoketones from ketones. All reactions were carried out under optimized reaction conditions and gave the target products in 61–95% yield.
{"title":"CuBr2 mediated synthesis of 2-Aminothiazoles from dithiocarbamic acid salts and ketones","authors":"Bao-Qiang Zhang, Lanxiang Shi","doi":"10.1080/10426507.2019.1633316","DOIUrl":"https://doi.org/10.1080/10426507.2019.1633316","url":null,"abstract":"Abstract In a one-pot procedure, CuBr2 has been used as a efficient desulfurizing agent in the synthesis of 2-aminothiazoles by the condensation of in situ-generated 1-substituted thioureas from their dithiocarbamic acid salts, with in situ-generated α-bromoketones from ketones. All reactions were carried out under optimized reaction conditions and gave the target products in 61–95% yield.","PeriodicalId":20043,"journal":{"name":"Phosphorus Sulfur and Silicon and The Related Elements","volume":"59 1","pages":"1134 - 1139"},"PeriodicalIF":0.0,"publicationDate":"2019-07-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75412811","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-03DOI: 10.1080/10426507.2019.1612147
Martin D. Rudd
{"title":"Foreword for international conference on the organic chemistry of sulfur, ISOCS-28","authors":"Martin D. Rudd","doi":"10.1080/10426507.2019.1612147","DOIUrl":"https://doi.org/10.1080/10426507.2019.1612147","url":null,"abstract":"","PeriodicalId":20043,"journal":{"name":"Phosphorus Sulfur and Silicon and The Related Elements","volume":"18 1","pages":"615 - 615"},"PeriodicalIF":0.0,"publicationDate":"2019-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88523559","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-01DOI: 10.1080/10426507.2019.1633320
Sevil Şenkardeş, I. Han, H. Hançer, Mürüvvet Abbak, Ö. Çevik, Ş. Güniz Küçükgüzel
Abstract A series of thiosemicarbazides were synthesized and structurally characterized by spectroscopic techniques (NMR, FT-IR) besides elemental analysis. These compounds were evaluated for their cytotoxicity against human breast cancer cell line MCF7 and prostate cancer cell line PC3 and nonmalignant fibroblast L929 cell line by MTT assay. Among the compounds, N-[2-(4-chlorophenyl)ethyl]-2-[(4-methylphenyl)sulfonyl]hydrazinecarbothioamide (3d) and 2-[(4-methylphenyl)sulfonyl]-N-[4-(trifluoromethoxy)phenyl]hydrazinecarbothioamide (3f) were found to display significant cytotoxicity with IC50 of 13.87 μM (against PC3 cell line) and 1.47 μM (against MCF7 cell line), respectively. These compounds were non-cytotoxic to normal cell line with IC50>100 μM. Western blotting studies demonstrated that compound 3f induced apoptosis and caused cell death in the MCF7 and PC3 cell lines via an increase in Bax protein expression and a slight decrease in Bcl-2 protein expression. The gene expression ratio Bax/Bcl-2 showed the induction of mitochondrial apoptosis in cancer cell lines. All of synthesized compounds have also been tested for antioxidant activity and all compounds achieved strong inhibition of the DPPH radical. These findings showed that compound 3f, displays potential to be further explored in the development of new anticancer agents. Graphical Abstract
{"title":"Synthesis, characterization and biological evaluation of some novel sulfonylthiosemicarbazides","authors":"Sevil Şenkardeş, I. Han, H. Hançer, Mürüvvet Abbak, Ö. Çevik, Ş. Güniz Küçükgüzel","doi":"10.1080/10426507.2019.1633320","DOIUrl":"https://doi.org/10.1080/10426507.2019.1633320","url":null,"abstract":"Abstract A series of thiosemicarbazides were synthesized and structurally characterized by spectroscopic techniques (NMR, FT-IR) besides elemental analysis. These compounds were evaluated for their cytotoxicity against human breast cancer cell line MCF7 and prostate cancer cell line PC3 and nonmalignant fibroblast L929 cell line by MTT assay. Among the compounds, N-[2-(4-chlorophenyl)ethyl]-2-[(4-methylphenyl)sulfonyl]hydrazinecarbothioamide (3d) and 2-[(4-methylphenyl)sulfonyl]-N-[4-(trifluoromethoxy)phenyl]hydrazinecarbothioamide (3f) were found to display significant cytotoxicity with IC50 of 13.87 μM (against PC3 cell line) and 1.47 μM (against MCF7 cell line), respectively. These compounds were non-cytotoxic to normal cell line with IC50>100 μM. Western blotting studies demonstrated that compound 3f induced apoptosis and caused cell death in the MCF7 and PC3 cell lines via an increase in Bax protein expression and a slight decrease in Bcl-2 protein expression. The gene expression ratio Bax/Bcl-2 showed the induction of mitochondrial apoptosis in cancer cell lines. All of synthesized compounds have also been tested for antioxidant activity and all compounds achieved strong inhibition of the DPPH radical. These findings showed that compound 3f, displays potential to be further explored in the development of new anticancer agents. Graphical Abstract","PeriodicalId":20043,"journal":{"name":"Phosphorus Sulfur and Silicon and The Related Elements","volume":"59 1","pages":"1164 - 1170"},"PeriodicalIF":0.0,"publicationDate":"2019-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78522002","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-06-28DOI: 10.1080/10426507.2019.1633323
Ali Irfan, Fozia Batool, Sajjad Ahmad, R. Ullah, Aeysha Sultan, R. Sattar, Bushra Nisar, Laila Rubab
Abstract 1,2,3-Thiadiazoles, structurally active pharmacophores have attracted significant attention of synthetic chemists, medicinal and pharmaceutical researchers because of their versatile biological activities against various diseases such as herbicidal, insecticidal, antiviral, antitumor, antimicrobial, anticancer, plants activator and anti-amoebic activities. A literature survey of the last decade presented in this review article summarizes the major synthetic approaches, methodologies and strategies adopted for the synthesis of 1,2,3-thiadiazole scaffolds which will be help for medicinal chemists and pharmacists in future synthesis and development of novel therapeutic agents. Graphical Abstract
{"title":"Recent trends in the synthesis of 1,2,3-thiadiazoles","authors":"Ali Irfan, Fozia Batool, Sajjad Ahmad, R. Ullah, Aeysha Sultan, R. Sattar, Bushra Nisar, Laila Rubab","doi":"10.1080/10426507.2019.1633323","DOIUrl":"https://doi.org/10.1080/10426507.2019.1633323","url":null,"abstract":"Abstract 1,2,3-Thiadiazoles, structurally active pharmacophores have attracted significant attention of synthetic chemists, medicinal and pharmaceutical researchers because of their versatile biological activities against various diseases such as herbicidal, insecticidal, antiviral, antitumor, antimicrobial, anticancer, plants activator and anti-amoebic activities. A literature survey of the last decade presented in this review article summarizes the major synthetic approaches, methodologies and strategies adopted for the synthesis of 1,2,3-thiadiazole scaffolds which will be help for medicinal chemists and pharmacists in future synthesis and development of novel therapeutic agents. Graphical Abstract","PeriodicalId":20043,"journal":{"name":"Phosphorus Sulfur and Silicon and The Related Elements","volume":"16 1","pages":"1098 - 1115"},"PeriodicalIF":0.0,"publicationDate":"2019-06-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81264510","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-06-27DOI: 10.1080/10426507.2019.1633318
A. Lozynskyi, B. Zimenkovsky, I. Ivasechko, J. Senkiv, A. Gzella, O. Karpenko, R. Stoika, R. Lesyk
Abstract The synthesis and anticancer activity evaluation of new thiazolo[4,5-b]pyridine-5-carboxylic acid amides is described. The structures of the synthesized compounds were confirmed by spectroscopic data and a single crystal X-ray diffraction analysis for 2.4. The synthesized compounds were screened for their in vitro anticancer activity according to US NCI protocols. The most active 7-(4-fluorophenyl)-2-oxo-2,3-dihydrothiazolo[4,5-b]pyridine-5-carboxylic acid (4-chlorophenyl)amide 2.2 and 7-(4-chlorophenyl)-2-oxo-2,3-dihydrothiazolo[4,5-b]pyridine-5-carboxylic acid (4-chlorophenyl)amide 2.5 were screened for their cytotoxicity effects on C6 Rat glioma cells and U373 Human glioblastoma astrocytoma cells which revealed promising results comparable to temozolamide as reference control according MTT assay data. GRAPHICAL ABSTRACT
{"title":"Synthesis and cytotoxicity of new 2-oxo-7-phenyl-2,3-dihydrothiazolo[4,5-b]pyridine-5-carboxylic acid amides","authors":"A. Lozynskyi, B. Zimenkovsky, I. Ivasechko, J. Senkiv, A. Gzella, O. Karpenko, R. Stoika, R. Lesyk","doi":"10.1080/10426507.2019.1633318","DOIUrl":"https://doi.org/10.1080/10426507.2019.1633318","url":null,"abstract":"Abstract The synthesis and anticancer activity evaluation of new thiazolo[4,5-b]pyridine-5-carboxylic acid amides is described. The structures of the synthesized compounds were confirmed by spectroscopic data and a single crystal X-ray diffraction analysis for 2.4. The synthesized compounds were screened for their in vitro anticancer activity according to US NCI protocols. The most active 7-(4-fluorophenyl)-2-oxo-2,3-dihydrothiazolo[4,5-b]pyridine-5-carboxylic acid (4-chlorophenyl)amide 2.2 and 7-(4-chlorophenyl)-2-oxo-2,3-dihydrothiazolo[4,5-b]pyridine-5-carboxylic acid (4-chlorophenyl)amide 2.5 were screened for their cytotoxicity effects on C6 Rat glioma cells and U373 Human glioblastoma astrocytoma cells which revealed promising results comparable to temozolamide as reference control according MTT assay data. GRAPHICAL ABSTRACT","PeriodicalId":20043,"journal":{"name":"Phosphorus Sulfur and Silicon and The Related Elements","volume":"2 1","pages":"1149 - 1157"},"PeriodicalIF":0.0,"publicationDate":"2019-06-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79560100","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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