Synthesis and biological evaluation of chalcones and their derived pyrazoles as potential cytotoxic agents

Bhat, Bilal A.; Dhar, K.L.; Puri, S. C.; Saxena, Ajit Kumar; Shanmugavel, M.; Qazi, Ghulam N.

doi:10.1016/j.bmcl.2005.03.121

Cited by 263 publications

(162 citation statements)

References 29 publications

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“…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

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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.

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Section: Introductionmentioning

confidence: 99%

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

Alex

Kumar

2013

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…22 C o n c e r n i n g t h e 1 -a r y l -1 H -p y r a z o l e -4 -carboximidamides compounds, the pyrazoles nucleus have displayed an impressive array of biological activities, among which antiprotozoa, anti-malarial, anti-inflammatory, immunomodulatory, nitric oxide inhibition, cytotoxic and anti-cancer activities. 23 …”

Section: Biological and Cytotoxity Assaysmentioning

confidence: 99%

Synthesis and antileishmanial activity of new 1-aryl-1H-pyrazole-4-carboximidamides derivatives

Santos¹,

Gomes²,

Bernardino³

et al. 2011

J. Braz. Chem. Soc.

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A quimioterapia para as leishmanioses, doenças causadas por protozoários do gênero Leishmania, ainda permanece ineficiente em diversos tratamentos. Portanto, existe a necessidade de pesquisa por novos fármacos. Nesse trabalho, foram sintetizados derivados 1-aril-1H-pirazol-4-carboximidamidas, avaliadas as atividades leishmanicida e os efeitos citotóxicos in vitro, e realizado um estudo de relação estrutura-atividade (REA) com a série de compostos. O composto 2 apresentou um perfil de atividade que pode ser melhorado através de estratégias de modificação molecular da química medicinal.Chemotherapy for leishmaniasis, diseases caused by protozoa of the genus Leishmania, remains inefficient in several treatments. So there is a need to search for new drugs. In this work, we have synthesized 1-aryl-1H-pyrazole-4-carboximidamides derivatives and evaluated antileishmanial activities in vitro, as well as cytotoxic effects. Structure-activity relationship (SAR) studies were carried out with all the compounds of the series. Compound 2 showed an activity profile that can be improved through medicinal chemistry strategies.

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“…[2] Dihydropyrimidines have attracted considerable attention as they appeared of interest to possess wide range of therapeutic activities. Different activities are as under antiviral [3][4] antibacterial [5] , antitumor [6][7] , cardiovascular [8][9] , anticarcinogenic [10] , antihypertensive…”

Section: Introductionmentioning

confidence: 99%