131507-32-9Relevant academic research and scientific papers
Design and synthesis of pyrazole–pyrazoline hybrids as cancer-associated selective COX-2 inhibitors
Akhtar, Wasim,Marella, Akranth,Alam, Mohammad Mumtaz,Khan, Mohemmed F.,Akhtar, Mymoona,Anwer, Tariq,Khan, Farah,Naematullah, Md.,Azam, Faizul,Rizvi, Moshahid A.,Shaquiquzzaman, Mohammad
, (2020/10/09)
In continuation of our previous work on cancer and inflammation, 15 novel pyrazole–pyrazoline hybrids (WSPP1–15) were synthesized and fully characterized. The formation of the pyrazoline ring was confirmed by the appearance of three doublets of doublets in 1H nuclear magnetic resonance spectra exhibiting an AMX pattern for three protons (HA, HM, and HX) of the pyrazoline ring. All the synthesized compounds were screened for their in vitro anticancer activity against five cell lines, that is, MCF-7, A549, SiHa, COLO205, and HepG2 cells, using the MTT growth inhibition assay. 5-Fluorouracil was taken as the positive control in the study. It was observed that, among them, WSPP11 was found to be active against A549, SiHa, COLO205, and HepG2 cells, with IC50 values of 4.94, 4.54, 4.86, and 2.09 μM. All the derivatives were also evaluated for their cytotoxicity against HaCaT cells. WSPP11 was also found to be nontoxic against normal cells (cell line HaCaT), with an IC50 value of more than 50 μM. The derivatives were also evaluated for their in vitro anti-inflammatory activity by the protein (egg albumin) denaturation assay and the red blood cell membrane stabilizing assay, using diclofenac sodium and celecoxib as standard. Compounds that showed significant anticancer and anti-inflammatory activities were further studied for COX-2 inhibition. The manifestation of a higher COX-2 selectivity index of WSPP11 as compared with other derivatives and an in vitro anticancer activity against four cell lines further established that compounds that were more selective toward COX-2 also exhibited a better spectrum of activity against various cancer cell lines.
Novel pyrazole-pyrazoline hybrids endowed with thioamide as antimalarial agents: Their synthesis and 3D-QSAR studies
Marella, Akranth,Shaquiquzzaman, Mohammad,Akhter, Mymoona,Verma, Garima,Alam, Mohammad Mumtaz
, p. 597 - 606 (2015/07/27)
One of the most viable options to tackle the growing resistance to the antimalarial drugs is hybrid molecules. It involves combination of different scaffolds in one frame that may lead to compounds with diverse biological profiles. In this context, new hybrids of three different scaffolds viz pyrazole, pyrazoline and thiosemicarbazone moiety were incorporated into one single compound and evaluated for their in vitro schizontocidal activity against the CQ-sensitive 3D7 strain of Plasmodium falciparum. Compounds with significant in vitro antimalarial activity were further evaluated for cytotoxicity against VERO cell lines. The best active compound 48 exhibited an IC50 of 1.13 μM. The in vitro results were further validated by quantitative structure-activity relationship (QSAR).
An efficient one-pot synthesis of some new 2,4-diaryl pyrido[3,2-c] coumarins as potent antimicrobial agents
Dawane, Bhaskar S.,Konda, Shankaraiah G.,Bodade, Ragini G.,Bhosale, Raghunath B.
experimental part, p. 237 - 241 (2010/04/24)
(Chemical Equation Presented) Poly(ethylene glycol) (PEG-400) has been used as sustainable, nonvolatile, and environmental friendly reaction solvent for the synthesis of title compounds. Various diaryl pyrido[3,2-c]coumarins have been synthesized in one s
