ChemInform Abstract: Convenient Access to New 4-Substituted Aminopyrido[2,3-d]pyrimidine Derivatives.

ChemInform ◽  
2016 ◽  
Vol 47 (9) ◽  
pp. no-no
Author(s):  
Fatima Belhadj ◽  
Zahira Kibou ◽  
Nawel Cheikh ◽  
Noureddine Choukchou-Braham ◽  
Didier Villemin
Keyword(s):  
Pyrimidine Derivatives ◽  
Convenient Access

Convenient access to new 4-substituted aminopyrido[2,3-d]pyrimidine derivatives

2015 ◽  
Vol 56 (44) ◽  
pp. 5999-6002 ◽  
Author(s):  
Fatima Belhadj ◽  
Zahira Kibou ◽  
Nawel Cheikh ◽  
Noureddine Choukchou-Braham ◽  
Didier Villemin
Keyword(s):  
Pyrimidine Derivatives ◽  
Convenient Access

Palladium-catalyzed carbonylative transformation of aryl iodides and sulfonyl chlorides: convenient access to thioesters

2020 ◽  
Vol 7 (6) ◽  
pp. 885-889 ◽  
Author(s):  
Xinxin Qi ◽  
Zhi-Peng Bao ◽  
Xiao-Feng Wu
Keyword(s):  
Sulfonyl Chlorides ◽  
Aryl Iodides ◽  
Palladium Catalyzed ◽  
Convenient Access

A palladium-catalyzed carbonylative transformation of aryl iodides and sulfonyl chlorides to thioesters has been studied.

Synthesis of Some New Tetracyclic Pyrimidine Derivatives Using Exocyclic α,β-Unsaturated Ketone and Evaluation of Their Antitumor Activities

2016 ◽  
Vol 12 (8) ◽  
pp. 311-317
Author(s):  
Kamelia El-Mahdy
Keyword(s):  
Antitumor Activity ◽  
Spectroscopic Data ◽  
Acid Hydrazide ◽  
Chloroacetic Acid ◽  
Equimolar Amount ◽  
Unsaturated Ketone ◽  
Cyanoacetic Acid ◽  
Antitumor Activities ◽  
Pyrimidine Derivatives ◽  
Cyanoacetic Acid Hydrazide

Thiazolopyrimidine 2 was obtained from the reaction of dihydropyrimidinone with chloroacetic acid and benzaldehyde. Thiazolopyrimidine 2 containing an α,β-unsaturated ketonic function [-CH=CH-CO-] has been used as a component of Michael addition with an equimolar amount of dinucleophiles to give a series of novel tetracyclic pyrimidine derivatives. Treatment of thiazolopyrimidine 2 with uracil, aminotriazole, cyanoacetic acid hydrazide, o-phenylenediamine or diaminopyridine afforded the corresponding pyridopyrimidine, triazolopyrimidine, pyrazolone, benzodiazepine and triazepine derivative, respectively. The detailed synthesis, spectroscopic data, and antitumor activity for synthesized compounds were reported.

An Update on JAK Inhibitors

2019 ◽  
Vol 26 (10) ◽  
pp. 1806-1832 ◽  
Author(s):  
Francesca Musumeci ◽  
Chiara Greco ◽  
Ilaria Giacchello ◽  
Anna Lucia Fallacara ◽  
Munjed M. Ibrahim ◽  
...  
Keyword(s):  
Clinical Trials ◽  
Tyrosine Kinases ◽  
Chemical Structure ◽  
Receptor Tyrosine Kinases ◽  
Myeloproliferative Neoplasms ◽  
Pharmaceutical Companies ◽  
Jak Inhibitors ◽  
Pyrimidine Derivatives ◽  
Janus Kinases ◽  
Structure Activity

Janus kinases (JAKs) are a family of non-receptor tyrosine kinases, composed by four members, JAK1, JAK2, JAK3 and TYK2. JAKs are involved in different inflammatory and autoimmune diseases, as well as in malignancies, through the activation of the JAK/STAT signalling pathway. Furthermore, the V617F mutation in JAK2 was identified in patients affected by myeloproliferative neoplasms. This knowledge prompted researchers from academia and pharmaceutical companies to investigate this field in order to discover small molecule JAK inhibitors. These efforts recently afforded to the market approval of four JAK inhibitors. Despite the fact that all these drugs are pyrrolo[2,3-d]pyrimidine derivatives, many compounds endowed with different heterocyclic scaffolds have been reported in the literature as selective or multi-JAK inhibitors, and a number of them is currently being evaluated in clinical trials. In this review we will report many representative compounds that have been published in articles or patents in the last five years (period 2013-2017). The inhibitors will be classified on the basis of their chemical structure, focusing, when possible, on their structure activity relationships, selectivity and biological activity. For every class of derivatives, compounds disclosed before 2013 that have entered clinical trials will also be briefly reported, to underline the importance of a particular chemical scaffold in the search for new inhibitors.

QSAR Studies of Halogenated Pyrimidine Derivatives as Inhibitors of Human Dihydroorotate Dehydrogenase Using Modified Bee Algorithm

2018 ◽  
Vol 21 (5) ◽  
pp. 381-387 ◽  
Author(s):  
Hossein Atabati ◽  
Kobra Zarei ◽  
Hamid Reza Zare-Mehrjardi
Keyword(s):  
External Validation ◽  
Correlation Coefficients ◽  
Quantitative Structure Activity Relationship ◽  
Molecular Structures ◽  
Dihydroorotate Dehydrogenase ◽  
Pyrimidine Derivatives ◽  
Qsar Studies ◽  
Bee Algorithm ◽  
Test Sets ◽  
Leave One Out

Aim and Objective: Human dihydroorotate dehydrogenase (DHODH) catalyzes the fourth stage of the biosynthesis of pyrimidines in cells. Hence it is important to identify suitable inhibitors of DHODH to prevent virus replication. In this study, a quantitative structure-activity relationship was performed to predict the activity of one group of newly synthesized halogenated pyrimidine derivatives as inhibitors of DHODH. Materials and Methods: Molecular structures of halogenated pyrimidine derivatives were drawn in the HyperChem and then molecular descriptors were calculated by DRAGON software. Finally, the most effective descriptors for 32 halogenated pyrimidine derivatives were selected using bee algorithm. Results: The selected descriptors using bee algorithm were applied for modeling. The mean relative error and correlation coefficient were obtained as 2.86% and 0.9627, respectively, while these amounts for the leave one out−cross validation method were calculated as 4.18% and 0.9297, respectively. The external validation was also conducted using two training and test sets. The correlation coefficients for the training and test sets were obtained as 0.9596 and 0.9185, respectively. Conclusion: The results of modeling of present work showed that bee algorithm has good performance for variable selection in QSAR studies and its results were better than the constructed model with the selected descriptors using the genetic algorithm method.

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