75403-98-4Relevant academic research and scientific papers
6-(Benzo1,3 dioxane)-4 phenylpyrimidamide derivative and preparation method and application thereof
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Paragraph 0040; 0098-0100, (2022/01/07)
The present invention discloses 6- (benzo 1,3 dioxane)-4 phenylpyrimidine amide derivative and preparation method and application thereof, said derivative having general formula I: wherein R is selected from H, halogen, alkyl and alkoxy, respectively; the
A Schmidt rearrangement-mediated synthesis of novel tetrahydro-benzo[1,4]diazepin-5-ones as potential anticancer and antiprotozoal agents
Insuasty, Daniel,Robledo, Sara M.,Vélez, Iván D.,Cuervo, Paola,Insuasty, Braulio,Quiroga, Jairo,Nogueras, Manuel,Cobo, Justo,Abonia, Rodrigo
, p. 567 - 583 (2017/11/03)
Novel tetrahydro-5H-benzo[e][1,4]diazepin-5-ones, several of them, containing the quinoline pharmacophore, were synthesized via a Schmidt rearrangement from their corresponding 1,2,3,4-tetrahydro-4-quinolones mediated by the NaN3/H2SO4 reaction conditions. Twelve of the obtained compounds were in vitro screened by the US National Cancer Institute (NCI) for their ability to inhibit 60 different human tumor cell lines, where compound 24a presented a remarkable activity against 58 of the 60 cancer cell lines, with the most important GI50 values ranging from 0.047 to 8.16 μM and LC50 values ranging from 9.4 to > 100 μM. Additionally, some of them were evaluated as antimalarial, antitrypanosomal and antileishmanial agents. The best antimalarial response was observed for compound 22g with an EC50 = 13.61 μg/mL for Plasmodium falciparum, while compound 24d exhibited high activity against Trypanosoma cruzi. and Leishmania (V) panamensis with EC50 = 2.78 μg/mL and 3.35 μg/mL respectively.
Synthesis and biological evaluation of substituted 4,6-diarylpyrimidines and 3,5-diphenyl-4,5-dihydro-1H-pyrazoles as anti-tubercular agents
Pathak, Vinay,Maurya, Hardesh K.,Sharma, Sandeep,Srivastava, Kishore K.,Gupta, Atul
supporting information, p. 2892 - 2896 (2014/06/10)
Various substituted 4,6-diarylpyrimidin-2-amine (4), 4,6-diaryl-2- (heteroaryl)pyrimidine (6) and 1-(3,5-diaryl-4,5-dihydro-1H-pyrazol-1-yl) ethanone (7) derivatives were synthesized in good yields using simple methodology. The synthesized compounds (4-7)
Synthesis of some pyrazolines and pyrimidines derived from polymethoxy chalcones as anticancer and antimicrobial agents
Rostom, Sherif A.F.,Badr, Mona H.,Abd El Razik, Heba A.,Ashour, Hayam M.A.,Abdel Wahab, Abeer E.
scheme or table, p. 572 - 587 (2012/07/03)
The synthesis of a series of certain polymethoxy chalcones and some derived pyrazole, pyrimidine, and thiazolopyrimidine ring structures is reported. Eleven compounds 4, 6, 9, 11, 14-17, 22, 24, and 25 were selected by the National Cancer Institute (NCI) to be screened for their in-vitro anticancer activity, whereas all the synthesized compounds were evaluated for their in-vitro antimicrobial activity. Compounds 4, 6, and 11 were found to possess a significant broad spectrum antitumor potential against most of the tested subpanel tumor cell lines. The pyrazolines 4 and 6 displayed remarkable growth inhibitory activities (GI50 MG-MID values of 2.10 and 1.38 μM, respectively), together with moderate cytostatic effects (TGI MG-MID values of 47.9 and 42.7 μM, respectively). Meanwhile, the pyrimidin-2-one 11 showed a noticeable overall tumor growth inhibitory activity, together with high cytostatic and cytotoxic efficacies (GI50, TGI and LC50 MG-MID values of 3.39, 17.4, and 61.7 μM, respectively). On the other hand, compounds 3, 4, 13, 15, 19, 20, and 23 were found to be the most active antimicrobial members in this investigation with a broad spectrum of activity. Compound 23 was four times superior to ampicillin against Pseudomonas aeruginosa. The best antifungal activity was demonstrated by compounds 4, 5, and 11 which possessed almost half the activity of clotrimazole against Candida albicans. Collectively, the obtained biological results suggest that compound 4 could be considered as a possible dual antimicrobial-anticancer agent. 22 novel compounds derived from polymethoxylated chalcones including dihydropyrazole, pyrimidine, and thiazolopyrimidine cyclized ring structures were synthesized, characterized, and evaluated for their biological activity as anticancer and/or antimicrobial agents. The results revealed that compounds 4, 6, and 11 were found to be the most active anticancer members with a significant broad spectrum antitumor potential against most of the tested subpanel tumor cell lines. Copyright
