74441-58-0Relevant articles and documents
Convenient synthesis and molecular docking of novel pyrido [2,3-d] pyrimidines as potent antimicrobial candidates
Mohamed, Hanaa S.,Nofal, Zeinab M.,Saleh, Abdulrahman M.,Sarhan, Alaadin E.
, p. 399 - 411 (2021/12/17)
New 3-(3,4-dimethoxyphenyl)-1-(thiophen-2-yl) prop-2-en-1-one has been designed as a starting compound to synthesis a novel series of substituted pyrido[2,3-d]pyrimidine system incorporated to different Schiff's bases and enamine derivatives as potent ant
Divergent Synthesis and Evaluation of the in vitro Cytotoxicity Profiles of 3,4-Ethylenedioxythiophenyl-2-propen-1-one Analogues
Karunakaran, Jayachandran,Dhatchana Moorthy, Nachiappan,Chowdhury, Somenath Roy,Iqbal, Saleem,Majumder, Hemanta K.,Gunasekaran, Krishnasamy,Vellaichamy, Elangovan,Mohanakrishnan, Arasambattu K.
, p. 1418 - 1430 (2019/08/07)
A new series of 3,4-ethylenedioxythiophene (EDOT)-appended propenones were prepared by condensation reaction and their in vitro cytotoxicity effects were evaluated against five human cancer cell lines. Preliminary structure–activity relationships of EDOT-
Chalcone derivatives targeting mitosis: synthesis, evaluation of antitumor activity and lipophilicity
Pinto, Patricia,Machado, Carmen Mariana,Moreira, Joana,Almeida, José Diogo P.,Silva, Patrícia M.A.,Henriques, Ana C.,Soares, José X.,Salvador, Jorge A.R.,Afonso, Carlos,Pinto, Madalena,Bousbaa, Hassan,Cidade, Honorina
, (2019/10/14)
This study describes the synthesis of a series of chalcones, including pyrazole and α,β-epoxide derivatives, and evaluation of their cell growth inhibitory activity in three human tumor cell lines, as well as their lipophilicity using liposomes as a biomi
Synthesis, molecular modeling, and biological evaluation of 4-[5-aryl-3-(thiophen-2-yl)-4,5-dihydro-1H-pyrazol-1-yl] benzenesulfonamides toward acetylcholinesterase, carbonic anhydrase I and II enzymes
Yamali, Cem,Gul, Halise Inci,Ece, Abdulilah,Taslimi, Parham,Gulcin, Ilhami
, p. 854 - 866 (2017/12/13)
In this study, 4-[5-aryl-3-(thiophen-2-yl)-4,5-dihydro-1H-pyrazol-1-yl] benzenesulfonamides were synthesized, and inhibition effects on AChE, hCA I, and hCA II were evaluated. Ki values of the compounds toward hCA I were in the range of 24.2?±?4.6-49.8?±?12.8?nm, while they were in the range of 37.3?±?9.0-65.3?±?16.7?nm toward hCA II. Ki values of the acetazolamide were 282.1?±?19.7?nm and 103.60?±?27.6?nm toward both isoenzymes, respectively. The compounds inhibited AChE with Ki in the range of 22.7?±?10.3-109.1?±?27.0?nm, whereas the tacrine had Ki value of 66.5?±?13.8?nm. Electronic structure calculations at M06-L/6-31?+?G(d,p)//AM1 level and molecular docking studies were also performed to enlighten inhibition mechanism and to support experimental findings. Results obtained from calculations of molecular properties showed that the compounds obey drug-likeness properties. The experimental and computational findings obtained in this study might be useful in the design of novel inhibitors against hCA I, hCA II, and AChE.
Synthesis of lignan conjugates via cyclopropanation: Antimicrobial and antioxidant studies
Raghavendra, Kanchipura Ramachandrappa,Renuka, Nagamallu,Kameshwar, Vivek H.,Srinivasan, Bharath,Ajay Kumar, Kariyappa,Shashikanth, Sheena
, p. 3621 - 3625 (2016/07/21)
Ethyl 2-(4-methoxyphenyl)-3-(thiophene-2-carbonyl)cyclopropanecarboxylates 2(a–f) and ethyl 4-aryl-7-oxo-4,5,6,7-tetrahydrobenzo[b]thiophene-5-carboxylates 4(a–f) were synthesized by simple procedure. The synthesized new compounds were screened in vitro for their antimicrobial and antioxidant activities. The compounds 2b and 4f showed excellent antibacterial activity; while 2b and 4f showed remarkable antifungal properties. The results of antioxidant activity studies revealed that compounds 4b and 4f manifested profound antioxidant potential. The docking studies were done for the final compounds. The ADME result indicates that all these molecules possess pharmaceutical properties in the range of 95% of drugs.
Discovery and structure activity relationships of 2-pyrazolines derived from chalcones from a pest management perspective
Kocyigit-Kaymakcloglu, Bedia,Beyhan, Nagihan,Tabanca, Nurhayat,Ali, Abbas,Wedge, David E.,Duke, Stephen O.,Bernier, Ulrich R.,Khan, Ikhlas A.
, p. 3632 - 3644 (2015/09/07)
Synthesis of chalcones and 2-pyrazoline derivatives has been an active field of research due to the established pharmacological effects of these compounds. In this study, a series of chalcone (1a-i), 2-pyrazoline-1-carbothioamides (2a-i), and 2-pyrazoline
Selected michael additions to thiophene-containing analogues of chalcone
Roman, Gheorghe
, p. 751 - 760 (2015/11/24)
Using thiophene-containing analogues of chalcone as substrates, a series of Michael additions were investigated. Thia-Michael addition of 4-chlorothiophenol led to 1-(substituted aryl)-3-(4-chlorophenylmercapto)-1-(2-thienyl)-1-propanones, whereas catalyt
Synthesis of manganese complexes of 4,5-dihydropyrazoles and metalation effect on the antimicrobial activity
Ahuja, Mamta
, p. 6443 - 6446 (2015/02/19)
1-Acetyl-5-aryl-3-(substituted thienyl)-4,5-dihydropyrazoles and their manganese complexes have been synthesized and characterized on the basis of elemental analysis, magnetic susceptibility, molar conductance, molecular weight determination and spectrosc
Synthesis and antibacterial activity of some heterocyclic chalcone analogues alone and in combination with antibiotics
Tran, Thanh-Dao,Nguyen, Thi-Thao-Nhu,Do, Tuong-Ha,Huynh, Thi-Ngoc-Phuong,Tran, Cat-Dong,Thai, Khac-Minh
experimental part, p. 6684 - 6696 (2012/08/28)
A series of simple heterocyclic chalcone analogues have been synthesized by Claisen Schmidt condensation reactions between substituted benzaldehydes and heteroaryl methyl ketones and evaluated for their antibacterial activity. The structures of the synthe
Synthesis of heterocyclic chalcone derivatives and their radical scavenging ability toward 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radicals
Hwang, Ki-Jun,Kim, Ho-Seok,Han, In-Cheol,Kim, Beom-Tae
, p. 2585 - 2591 (2012/10/29)
A series of heterocyclic chalcone derivatives bearing heterocycles such as thiophene or furan ring as an isostere of benzene ring were carefully prepared, and the influence of heterocycles on 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activit
