177984-97-3Relevant academic research and scientific papers
Synthesis and cytotoxicity studies of 3,5-diaryl N-acetyl pyrazoline - Isatin hybrids
Sharma, Manmohan,Sharma, Sahil,Buddhiraja, Abhishek,Saxena,Nepali, Kunal,Bedi
, p. 4337 - 4344 (2014)
Numerous reports highlighting the cytotoxic effects of 3,5-diaryl N-acetyl-pyrazolines and isatin tempted us to synthesise conjugates of the functionalities via alkyl armed triazole tetheration. The hybrids were synthesized by click chemistry approach and were evaluated against a panel of cell lines i.e. viz HeLa (cervix cancer), CAKI-I (Renal cancer), PC-3 (Prostate cancer) and Mia-paca-2 (pancreatic cancer). The hybrids were classified into right-handed and left-handed conjugates on the basis of the placement of the isatin ring. The length of the alkyl armed triazole linker was varied from 2 to 6. Structure activity relationship has also been presented. A preliminary cytotoxic assay was performed on the series of 3,5-diaryl N-acetyl-pyrazolines and only the potent 3,5-diaryl N-acetylpyrazolines were selected for their inclusion in the hybrid scaffold. Among the cell lines employed, HeLa cell line was the most sensitive towards the exposure of test compounds. Out of all the compounds evaluated, two right-handed conjugates MI-7b and MI-8b and two left-handed conjugates MI-4b, MI-6b displayed significant cytotoxic potential and exhibited an IC50 range from 1.3 to 3.5 μM against HeLa Cell line.
Facile Microwave-assisted Synthesis of 1,3,5-Trisubstituted Pyrazoline Derivatives Incorporating Sulfonyl Moiety
Liu, Fei,Yang, Jin-Feng,Liu, Hong,Wei, Wen-Zhen,Ma, Yan-Mei
, p. 254 - 260 (2016/04/19)
We developed an environmentally benign, convenient microwave-assisted process for the construction of 1,3,5-trisubstitued pyrazolines (10a～10f, 11a～11f, 12a～12f, 13a～13f). Chalcones, as the key intermedi- ates, were obtained by the condensation of each of appropriately substituted aromatic aldehydes (1～4) with 4-substituted acetophenones (5a～5f) via a Claisen-Schmidt reaction under the action of microwave irradiation. Cyclization of the chalcones (6a～6f, 7a～7f, 8a～8f, 9a～9f) with p-toluene sulfonhydrazide af- forded 1,3,5-trisubstitued pyrazoline derivatives using microwave-assisted process in 25 min and 140 watt power in glycol. The structures of targeted compounds were established by IR, 1H NMR, MS and ele- mental analysis. The results indicate that microwave-assisted synthetic process presents advantages in terms of enhancement in rate, decrease in reaction time, clean reaction and convenient operation.
Synthesis and biological activity of 4,6-substituted aryl-1-acetyl pyrimidine-2-ols
Bamnela, Rita,Shrivastava
experimental part, p. 6553 - 6558 (2010/12/25)
The synthesis of 4-(4'-bromophenyl)-6-substituted aryl-1-acetyl-pyrimidine-2-ols have been reported. The synthesized derivatives were characterized by elemental analysis and spectral data (IR and 1H NMR). All the synthesized derivatives have been evaluated for their antimicrobial and anthelmintic activities against microbes and helminthes.
Synthesis and In vitro antimicrobial, anthelmintic and insecticidal activities study of 4(4'-bromophenyl)-6-substituted-aryl-1-acetyl pyrimidine-2-thiols
Bamnela, Rita,Shrivastava
experimental part, p. 935 - 941 (2011/12/04)
A new series of 4(4'-bromophenyl)-6-substituted aryl-1-acetyl pyrimidine-2-thiol derivatives were synthesized by heating chalcones with thiourea, in the presence of ethanolic potassium hydroxide, followed by treatment with acetyl chloride. The structure of the compounds was characterized by IR and H1 NMR spectral study and elemental analysis. The compounds were screened for their antimicrobial, anthelmintic and insecticidal activities. All the compounds exhibited significant to moderate biological activities.
