229015-76-3Relevant articles and documents
A new synthetic approach for pyrazolo[1,5-a]pyrazine-4(5H)-one derivatives and their antiproliferative effects on lung adenocarcinoma cell line
Uygun, Meltem Tan,Amudi, Karina,Tura?l?, ?rem Do?an,Menges, Nurettin
, (2021/01/11)
Abstract: Starting from the 3,5-dimethyl pyrazole ring and acetophenone derivatives, five different N-propargylated C-3 substituted pyrazoles were obtained. These derivatives were reacted with different amine derivatives using Cs2CO3 in methanol and 11 different pyrazolo [1,5-a] pyrazine-4(5H)-one derivatives were obtained, which are not found in the literature. The cytotoxic effects of these derivatives in the A549 cell line were investigated. The 160?μM concentration of two derivatives was found to increase cell death rate to 50%, and two derivatives increased cell death rate by up to 40%. The structure–activity relationship (SAR) study revealed an amide group with a long alkyl chain and benzene ring with a p-CF3 group could be important for efficiency. With theoretical ADMET studies of pyrazolopyrazine derivatives, pharmacokinetic phases were predicted to be suitable. Graphic abstract: [Figure not available: see fulltext.].
Synthesis, Characterization and biological applications of pyrazole-benzothiazolamine conjugates
Sharma, Ramayanam S.K.,Kumar, Ramachandrula Krishna,Ravi Kumar,Havele, Shrikanth H.,Murali Mohan Rao
, p. 1029 - 1034 (2017/03/22)
Present paper describes the synthesis of some new pyrazole-benzothiazolamine conjugates by molecular conjunction by adopting appropriate synthetic routes. Purification of intermediates and final compounds has been done by recrystallization and chromatographic techniques. Characterization of all the newly synthesized pyrazole-benzothiazolamine derivatives was done by physical and spectral data. The experimental procedure for the preparation of seventeen pyrazole-benzthiazolamine conjugates has been incorporated. Data of synthesized compounds like IR, 1H NMR and Mass spectra were neatly presented. All these compounds were evaluated for their activity against Gram-positive and Gram-negative bacteria and various fungal strains. Anticancer activity has been carried out for the synthesized compounds using HeLa, DU145 and A549 cell lines using MTT assay and we found that the pyrazole-benzothiazolamine conjugates were possess antimicrobial, antifungal and anticancer activities.
Design, synthesis and biological evaluation of novel pyrazolochalcones as potential modulators of PI3K/Akt/mTOR pathway and inducers of apoptosis in breast cancer cells
Shaik, Anver Basha,Rao, Garikapati Koteswara,Kumar, G. Bharath,Patel, Nibeditha,Reddy, Vangala Santhosh,Khan, Irfan,Routhu, Sunitha Rani,Kumar, C. Ganesh,Veena, Immadi,Chandra Shekar, Kunta,Barkume, Madan,Jadhav, Shailesh,Juvekar, Aarti,Kode, Jyoti,Pal-Bhadra, Manika,Kamal, Ahmed
, p. 305 - 324 (2017/08/14)
Cancer has been established as the “Emperor of all maladies”. In recent years, medicinal chemistry has focused on identifying novel anti-cancer compounds; though discovery of these compounds appears to be a herculean task. In present study, we synthesized
On water synthesis of N-unsubstituted pyrazoles: Semicarbazide hydrochloride as an alternative to hydrazine for preparation of pyrazole-3-carboxylate derivatives and 3,5-disubstituted pyrazoles
Markovi, Violeta,Joksovi, Milan D.
supporting information, p. 842 - 847 (2015/03/04)
A green, simple and highly efficient method for the synthesis of pyrazole-3-carboxylates and 3,5-disubstituted pyrazoles by cyclization of 4-aryl(hetaryl, alkyl)-2,4-diketoesters and 1,3-diketones with semicarbazide hydrochloride under on water conditions has been developed. This method also does not require toxic hydrazine and product purification, eliminating the use of toxic liquid chemicals.
Novel heteroarylcarboxamide derivative or pharmacutically acceptable salt thereof, process for the preparation thereof and pharmaceutical composition for prevention or treatment of RAGE receptor related diseases containing the same as an active ingredient
-
Paragraph 0365; 0369-0370, (2021/11/02)
The present invention refers to novel heterocyclic biting Carbox probably the id derivative acceptable salt, and manufacturing method thereof including RAGE associated active acetylcholinesterase receptor or pharmaceutical composition for preventing or treating disease is directed to. Heterocycle by the present invention a derivative biting Carbox probably the id RAGE receptor antagonism in by, nerve cells with the beta loss oh with wheat id RAGE conjunction with receptor, inhibiting moving into brain, the resulting beta Amyloid plaque formed 21 is known to effectively inhibit generation.. Furthermore, memory a chemicals that are important in the acetylcholine for decomposing an aromatic thus inhibiting acetylcholine s reel sacrifice , RAGE disease associated active acetylcholinesterase receptor or Alzheimer's disease, cerebrovascular dementia, dementia due to damage bean curd, multi blockade dementia, Alzheimer's disease or the like dementia alcoholic or mixed dementia multi blockade and including dementia, pick (pick) bottle, a smartcrew [...] -Jakob (Creutzfeldt-jakob) bottle, that thyroid gland symptoms , bean curd a blade Parkinson (Parkinson) bottle, Huntington's disease (Huntington) which is useful in preventing or treating, can be used.
Synthesis of arylpyrazole linked benzimidazole conjugates as potential microtubule disruptors
Kamal, Ahmed,Shaik, Anver Basha,Polepalli, Sowjanya,Kumar, G. Bharath,Reddy, Vangala Santhosh,Mahesh, Rasala,Garimella, Srujana,Jain, Nishant
, p. 1082 - 1095 (2015/03/04)
In an attempt to develop potent and selective anticancer agents, a series of twenty arylpyrazole linked benzimidazole conjugates (10a-t) were designed and synthesized as microtubule destabilizing agents. The joining of arylpyrazole to the benzimidazole mo
Design and synthesis of pyrazole-oxindole conjugates targeting tubulin polymerization as new anticancer agents
Kamal, Ahmed,Shaik, Anver Basha,Jain, Nishant,Kishor, Chandan,Nagabhushana, Ananthamurthy,Supriya, Bhukya,Bharath Kumar,Chourasiya, Sumit S.,Suresh, Yerramsetty,Mishra, Rakesh K.,Addlagatta, Anthony
, p. 501 - 513 (2015/01/30)
A series of twenty one compounds with pyrazole and oxindole conjugates were synthesized by Knoevenagel condensation and investigated for their antiproliferative activity on different human cancer cell lines. The conjugates are comprised of a four ring scaffold; the structural isomers 12b and 12c possess chloro-substitution in the D ring. Among the congeners 12b, 12c, and 12d manifested significant cytotoxicity and inhibited tubulin assembly. Treatments with 12b, 12c and 12d resulted in accumulation of cells in G2/M phase, disruption of microtubule network, and increase in cyclin B1 protein. Zebrafish screening revealed that 12b, and 12d caused developmental defects. Docking analysis demonstrated that the congeners occupy the colchicine binding pocket of tubulin.
Design and synthesis of pyrazole/isoxazole linked arylcinnamides as tubulin polymerization inhibitors and potential antiproliferative agents
Kamal, Ahmed,Shaik, Anver Basha,Rao, Bala Bhaskara,Khan, Irfan,Bharath Kumar,Jain, Nishant
, p. 10162 - 10178 (2015/10/28)
As pyrazole and isoxazole based derivatives are well-known for displaying a considerable biological profile, an attempt has been made to unravel their cytotoxic potential. In this context, a number of pyrazole/isoxazole linked arylcinnamide conjugates (15
Cascade regioselective synthesis of pyrazoles from nitroallylic acetates and N-tosyl hydrazine
Shao, Nana,Chen, Tong,Zhang, Taotao,Zhu, Huajian,Zheng, Qunxiong,Zou, Hongbin
, p. 795 - 799 (2014/01/23)
A simple, practical, and regioselective synthetic protocol for the formation of pyrazoles was developed. Unlike all other previously reported reactions of nitroallylic acetates, this process was initiated by a S N2 reaction at the electrophilic γ site. A plausible mechanism for the cascade SN2-Michael synthesis is proposed.
