306936-57-2

Usage

Chemical Properties

White to yellow-orange solid

InChI:InChI=1/C10H7FN2O/c11-9-3-1-7(2-4-9)10-8(6-14)5-12-13-10/h1-6H,(H,12,13)

Upstream product

• 120445-82-1 (E)-2-(1-(4-fluorophenyl)ethylidene)hydrazinecarboxamide 
• 68-12-2 N,N-dimethyl-formamide 
• 326-33-0 4-fluoroacetophenone semicarbazone 
• 403-42-9 1-(4-fluorophenyl)ethanone 

Downstream Products

• 1001610-16-7 13-[3-(4-fluorophenyl)-1H-pyrazol-4-yl]-7,13-dihydro-12H-benzo[f]indeno[1,2-b]quinolin-12-one 
• 881667-24-9 2-[3-(4-fluoro-phenyl)-1H-pyrazol-4-yl]-3-(3-methoxy-propyl)-thiazolidin-4-one 
• 484049-75-4 2-[3-(4-fluorophenyl)-1H-pyrazol-4-yl]-methylene-1,3-indandione 

Relevant academic research and scientific papers

Synthesis of lathyrane diterpenoid nitrogen-containing heterocyclic derivatives and evaluation of their anti-inflammatory activities

As our ongoing work on lathyrane diterpenoid derivatization, three series of lathyrane diterpenoid derivatives were designed and synthesized based combination principles, including pyrazole, thiazole and furoxan moieties. Biological evaluation indicated t

Synthesis and evaluation of antimicrobial and anticancer activities of 3-phenyl-1-phenylsulfonyl pyrazoles containing an aminoguanidine moiety

A series of 3-phenyl-1-phenylsulfonyl pyrazoles containing an aminoguanidine moiety was designed, synthesized, and evaluated for their antimicrobial and anticancer activities. The majority of the target compounds showed broad-spectrum antimicrobial activi

Synthesis and biological evaluation of some pyrazole derivatives, containing (Thio) semicarbazide, as dual anti-inflammatory antimicrobial agents

Background: Several series of pyrazole derivatives containing (thio) semicarbazide (4a-4h, 5a-5l, 6a-6f, 7a-7c) were designed and synthesized to screen dual inflammatory and antimicrobial activities. Methods: The products were characterized by1

Synthesis and the interaction of 2-(1H-pyrazol-4-yl)-1H-imidazo[4,5-f][1,10]phenanthrolines with telomeric DNA as lung cancer inhibitors

A novel series of 2-(1H-pyrazol-4-yl)-1H-imidazo[4,5-f][1,10]phenanthrolines were designed, synthesized and evaluated for their antitumor activity against lung adenocarcinoma by CCK-8 assay, electrophoretic mobility shift assay (EMSA), UV-melting study, wound healing assay and docking study. These compounds showed good inhibitory activities against lung adenocarcinoma. Especially compound 12c exhibited potential antiproliferative activity against A549?cell line with the half maximal inhibitory concentration (IC50) value of 1.48?μM, which was a more potent inhibitor than cisplatin (IC50?=?12.08?μM) and leading compound 2 (IC50?=?1.69?μM), and the maximum cell inhibitory rate being up to 98.40%. Moreover, further experiments demonstrated that compounds 12a–d can strongly interact with telomeric DNA to stabilize G-quadruplex DNA with increased ΔTm values from 12.44 to 20.54?°C at a ratio of DNA to compound 1:10. These results implied that growth inhibition of A549?cells mediated by these phenanthroline derivatives is possibly positively correlated to the fact their interaction with telomeric G-quadruplexs.

Synthesis and antimicrobial evaluation of (Z)-5-((3-phenyl-1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one derivatives

Background: An alarming increment in pathogenic resistance to existing anti-microbial agents is a serious problem and the treatment of these bacterial infections is becoming increasingly challenging. Therefore, there is an urgent need to develop novel ant

Synthesis and antitubercular and antibacterial activity of some active fluorine containing quinoline–pyrazole hybrid derivatives

In an attempt to develop newer antitubercular and antibacterial agents against the increasing bacterial resistance, we have designed new quinoline–pyrazole analogs (8a–u) following the molecular hybridization approach. The structure of one of the final compounds, 8a was unambiguously confirmed by single crystal X-ray diffraction (SC-XRD) analysis. The target compounds were evaluated for their antitubercular activity against Mycobacterium tuberculosis and antibacterial activity against three common pathogenic bacterial strains. Four derivatives (8b, 8c, 8j and 8o) displayed significant antitubercular activity. The compounds derived from 8-trifluoromethylquinoline and 6-fluoroquinoline scaffolds with halogen substitution on the pyrazole ring exhibited superior inhibition activity than corresponding 6-methoxyquinoline analogs. The cytotoxic studies revealed that the active compounds are nontoxic to normal Vero cell lines with selectivity index values ≥10, which indicate the suitability of these compounds for further drug development. The in silico molecular docking study demonstrated strong binding affinity of the compounds with the target enzymes (InhA, CYP121 and TMPK) of M. tuberculosis. Further, the in vitro antibacterial activity of compounds 8b, 8c, 8d and 8g is comparable with that of the reference drug, Ciprofloxacin.

ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF

Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.

PREPARATION AND METHODS OF USE FOR ORTHO-ARYL 5- MEMBERED HETEROARYL-CARBOXAMIDE CONTAINING MULTI-TARGETED KINASE INHIBITORS

The present disclosure relates to compounds of the Formula (I): and pharmaceutically acceptable salts, as kinase modulators, compatible with the Type-II inhibition of kinases.

UNSATURATED HETEROCYCLIC INHIBITORS OF NECROPTOSIS

The invention features new small molecule inhibitors of necroptosis. The compounds of the invention are described by Formulas (I) and (II). The invention also features pharmaceutical compositions that include compounds of Formula (I) and (II). The compounds and compositions of the invention are also featured in kits and in methods of treatment of conditions that include neurodegenerative diseases, ischemic brain and heart injuries, and head trauma.

Structure-activity relationship study of a novel necroptosis inhibitor, necrostatin-7

Necroptosis is a regulated caspase-independent cell death mechanism characterized by morphological features resembling non-regulated necrosis. Necrotatin-7 (Nec-7), a novel potent small-molecule inhibitor of necroptosis, is structurally distinct from previously described necrostatins (Nec-1, Nec-3, Nec-4 and Nec-5). Here, we describe a series of structural modifications and the structure-activity relationship (SAR) of the Nec-7 series for inhibiting necroptosis.