42062-89-5Relevant academic research and scientific papers
Synthesis and in vitro anticancer activity of novel heterocycles utilizing thiophene incorporated thioureido substituent as precursors
Abdel-Motaal, Marwa,Alanzy, Asmaa L.,Asem, Medhat
, p. 560 - 569 (2020/07/31)
Ethyl 2-(3-allylthioureido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylate (1) was used as a building block for synthesis of new heterocycles. Pyrimidine and thiazole moieties were achieved upon condensation of compound 1 with various reagents such as chloroacetic acid, dietyl malonate, ninhydrin, 2,3-epoxy-2,3-dihydro-1,4-naphthoquinone, and hydrazine hydrate. The structures of the newly synthesized compounds were confirmed using spectral measurements. The prepared products were evaluated for their anticancer activity against colon HCT-116 human cancer cell line. Compounds 6, 9, 10a, 11, 12, 15 have displayed potent activity.
Design, synthesis, molecular docking and biological evaluation of thiophen-2-iminothiazolidine derivatives for use against Trypanosoma cruzi
Silva-Júnior,Silva,Fran?a,Silva,Barreto,Silva,Ferreira,Gatto,Moreira,Siqueira-Neto,Mendon?a-Júnior,Lima,Bortoluzzi,Scotti,Scotti,Meneghetti,Aquino,Araújo-Júnior
, p. 4228 - 4240 (2016/08/23)
In this study, we designed and synthesized a series of thiophen-2-iminothiazolidine derivatives from thiophen-2-thioureic with good anti-Trypanosoma cruzi activity. Several of the final compounds displayed remarkable trypanocidal activity. The ability of the new compounds to inhibit the activity of the enzyme cruzain, the major cysteine protease of T. cruzi, was also explored. The compounds 3b, 4b, 8b and 8c were the most active derivatives against amastigote form, with significant IC50values between 9.7 and 6.03?μM. The 8c derivative showed the highest potency against cruzain (IC50?=?2.4?μM). Molecular docking study showed that this compound can interact with subsites S1 and S2 simultaneously, and the negative values for the theoretical energy binding (Eb?=??7.39?kcal·mol?1) indicates interaction (via dipole–dipole) between the hybridized sulfur sp3atom at the thiazolidine ring and Gly66. Finally, the results suggest that the thiophen-2-iminothiazolidines synthesized are important lead compounds for the continuing battle against Chagas disease.
Heterocyclization of 5,6-disubstituted 3-alkenyl-2-thioxothieno[2,3-d]pyrimidin-4-one with p-alkoxyphenyltellurium trichloride
Kut, Mykola,Onysko, Mikhajlo,Lendel, Vasyl
, p. 347 - 350 (2016/12/16)
Electrophilic heterocyclization of 5,6-disubstituted 3-alkenyl-2-thioxothieno[2,3-d]pyrimidin-4-ones by treatment with p-alkoxyphenyltellurium trichlorides leads to annulation of the thiazoline moiety with the formation of 6,7-disubstituted-2-[dichloro-(p-alkoxyphenyl)telluromethyl]-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]thieno[2,3-d]pyrimidin-5-one hydrochlorides.
2-(3,4-dihydro-4-oxothieno[2,3-d]pyrimidin-2-ylthio) acetamides as a new class of falcipain-2 inhibitors. 3. design, synthesis and biological evaluation
Zhu, Jin,Chen, Tong,Liu, Jie,Ruoqun, Ma.,Lu, Weiqiang,Huang, Jin,Li, Honglin,Li, Jian,Jiang, Hualiang
body text, p. 785 - 797 (2009/05/27)
The cysteine protease falcipain-2 (FP-2) of Plasmodium falciparum is a principal cysteine protease and an essential hemoglobinase of erythrocytic P. falciparum trophozoites, making it become an attractive target enzyme for developing anti-malarial drugs.
Synthesis and transformations of 3-ethoxycarbonyl-2-(N-R-thioreido)thiophenes
Chumakova,Demchenko,Krasovsky,Dolishnyak,Lozinskii
, p. 1002 - 1012 (2007/10/03)
3-Ethoxycarbonyl-2-N-R-thioureido)-4,5,6,7-tetrahydrobenzo[b]thiophenes were obtained by the reaction of 2- amino-3-ethoxycarbonyl-4,5,6,7-tetrahydrobenzo[b]thiophene with isothiocyanates and of 3-ethoxycarbonyl-2-isothiocyanato-4,5,6,7-tetrahydrobenzo[b]
Synthesis of 3 substituted thieno[2,3 d]pyrimidin 4(3H) one 2 mercaptoacetic acids and their ethyl esters for pharmacological screening
Devani,Shishoo,Pathak,Parikh,Shah,Padhya
, p. 660 - 664 (2007/10/08)
3 Substituted thieno[2,3 d]pyrimidin 4(3H) one 2 mercaptoacetic acids and their ethyl esters were synthesized from 2 mercaptothieno[2,3 d]pyrimidin 4 (3H) ones, which were obtained by cyclization of thienylthioureas in acidic medium. Analgesic, anti inflammatory, and anticonvulsant activities were found in some of these compounds. Significant antimicrobial activity was exhibited by thienylthioureas.
