Design, synthesis, and biological testing of pyrazoline derivatives of combretastatin-A4

Johnson, Marlie A.; Younglove, Brent; Lee, Lauren; LeBlanc, Regan M.; Holt, Herman L.; Hills, Patrice; Mackay, Hilary; Brown, Toni; Mooberry, Susan L.; Lee, Moses

doi:10.1016/j.bmcl.2007.07.105

Cited by 147 publications

(78 citation statements)

References 28 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Many pyrazole derivatives are reported to have a broad spectrum of biological activities, such as anti-inflammatory [13], antifungal [14], antiviral [15], cytotoxic [12], A3 adenosine receptor antagonists [16], antioxidant [13], antihypertensive [17], tranquilizing, muscle relaxant, psychoanaleptic, hypnotic, ulcerogenic, antidepressant, antibacterial and analgesic effects [18]. Pharmacologically-interesting heterocyclic systems like pyrazolines have been widely studied owing to their pharmacological activities, which include anti-tumor [19,20], anti-inflammatory [21][22][23][24][25][26][27][28][29][30][31][32], anti-parasitary [33], anticonvulsant [34], antimicrobial [35][36][37][38][39], antinociceptives [40], antimalarial [41], nitric oxide synthase inhibitory, associated with diseases such as Alzheimer, Huntington, and inflammatory arthritis [42], antidepressant [43,44], anticancer [45][46][47], antibacterial [48], antitubercular, analgesic [49], antiviral [46], antioxidant [50], antiamoebic …”

Section: Introductionmentioning

confidence: 99%

Synthesis, Antibacterial and Antifungal Activity of Some New Pyrazoline and Pyrazole Derivatives

Hassan

2013

Molecules

142

View full text Add to dashboard Cite

A series of 2-pyrazolines 5-9 have been synthesized from α,β-unsaturated ketones 2-4. New 2-pyrazoline derivatives 13-15 bearing benzenesulfonamide moieties were then synthesized by condensing the appropriate chalcones 2-4 with 4-hydrazinyl benzenesulfonamide hydrochloride. Ethyl [1,2,4] Condensation of 6,6-dimethyl-4-oxo-4,5,6,7-tetrahydro-1H-indole-2-carbaldehyde (1') with compound 24 or 25 afforded the corresponding Schiff's bases 36 and 37, respectively. Reaction of the Schiff's base 37 with benzoyl hydrazine or acetic anhydride afforded benzohydrazide derivative 39 and the cyclized compound 40, respectively. Furthermore, the pyrazole derivatives 42-44 were synthesized by cyclization of hydrazine derivative 25 with the prepared chalcones 2-4. All the newly synthesized compounds have been characterized on the basis of IR and 1 H-NMR spectral data as well as physical data.Antimicrobial activity against the organisms E. coli ATCC8739 and P. aeruginosa ATCC 9027 as examples of Gram-negative bacteria, S. aureus ATCC 6583P as an example of Gram-positive bacteria and C. albicans ATCC 2091 as an example of a yeast-like fungus have been studied using the Nutrient Agar (NA) and Sabouraud Dextrose Agar (SDA) diffusion methods. The best performance was found for the compounds 16, 17, 19 and 20.

show abstract

Section: Introductionmentioning

confidence: 99%

Synthesis, Antibacterial and Antifungal Activity of Some New Pyrazoline and Pyrazole Derivatives

Hassan

2013

Molecules

142

View full text Add to dashboard Cite

show abstract

“…The presence of this moiety in several therapeutically active compounds encouraged the researchers in the direction of design and synthesis of novel pyrazoline derivatives possessing myriad activities. Some of the activities that pyrazolines exhibit are anticancer 20,21 , antitumor 22 , anti-androgenic 23 , antioxidant 24 , antimicrobial [25][26][27] , antiviral 28 , antitubercular 29,30 , antimalarial 31 , anti-amoebic 32,33 , COX-II 34,35 , monoamine oxidase 36,37 , xanthine oxidase 38 and amine oxidase 39 inhibitory, and so on. With an incentive to improve the existing activities several modifications are being done on this scaffold and many of which are proved to be successful.…”

Section: Introductionmentioning

confidence: 99%

4,5-Dihydro-1H-pyrazole: an indispensable scaffold

Alex

Kumar

2013

Journal of Enzyme Inhibition and Medicinal Chemistry

View full text Add to dashboard Cite

Pyrazoles, categorized as nitrogen-containing heterocycles, are well known for their interminable participation in the field of perpetual research and development of therapeutical active agents. As a consequence pyrazoles became an inevitable core of numerous drugs having diverse activities. The broad spectrum of activities portrayed by the pyrazoles instigated the researchers to modify the pyrazole ring as 4,5-dihydro-1H-pyrazoles commonly known as 2-pyrazolines. The present review is a concerted effort to retrace compounds covered from 2009-till date which owe diverse biological activities to the 2-pyrazoline scaffold and also condenses the retro-synthetic approaches employed for their synthesis. This endeavor culminated in revelation that inhibitory potential varied when the substituents in particular N-substituents of 2-pyrazolines were altered.

show abstract

“…Pyrazoline derivatives have been reported to exhibit a wide spectrum of biological effects including anticancer activity [6][7][8][9][10][11][12][13][14][15][16] . Some compounds bearing pyrazole moiety exert their therapeutic action by inhibiting different types of enzymes that play important roles in cell division [16][17][18] .…”

Section: Introductionmentioning

confidence: 99%

Synthesis of 1-acetyl-3-(2-thienyl)-5-aryl-2-pyrazoline derivatives and evaluation of their anticancer activity

Özdemir

Altıntop

Kaplancıklı

et al. 2012

Journal of Enzyme Inhibition and Medicinal Chemistry

View full text Add to dashboard Cite

show abstract

Design, synthesis, and biological testing of pyrazoline derivatives of combretastatin-A4

Cited by 147 publications

References 28 publications

Synthesis, Antibacterial and Antifungal Activity of Some New Pyrazoline and Pyrazole Derivatives

Synthesis, Antibacterial and Antifungal Activity of Some New Pyrazoline and Pyrazole Derivatives

4,5-Dihydro-1H-pyrazole: an indispensable scaffold

Synthesis of 1-acetyl-3-(2-thienyl)-5-aryl-2-pyrazoline derivatives and evaluation of their anticancer activity

Contact Info

Product

Resources

About