Journal ArticleDOI
Synthesis of some pyrazole derivatives and preliminary investigation of their affinity binding to P-glycoprotein.
Fedele Manna,Franco Chimenti,Rossella Fioravanti,Adriana Bolasco,Daniela Secci,Paola Chimenti,Cristiano Ferlini,Giovanni Scambia +7 more
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TLDR
A series of substituted pyrazolines were synthesized and evaluated for their anticancer activity and for their ability to inhibit P-glycoprotein-mediated multidrug resistance by direct binding to a purified protein domain containing an ATP-binding site and a modulator interacting region.About:
This article is published in Bioorganic & Medicinal Chemistry Letters.The article was published on 2005-10-15. It has received 121 citations till now. The article focuses on the topics: Pyrazole.read more
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Synthesis of new 4-thiazolidinone-, pyrazoline-, and isatin-based conjugates with promising antitumor activity.
Dmytro Havrylyuk,Borys Zimenkovsky,Olexandr Vasylenko,Andrzej Gzella,Andrzej Gzella,Roman Lesyk +5 more
TL;DR: The most effective anticancer compound 10 was found to be active with mean GI₅₀ and TGI values of 0.071 μM and 0.76 μM, respectively and demonstrated the highest antiproliferative influence on the non-small-cell lung cancer cell line HOP-92.
Journal ArticleDOI
Biological activities of pyrazoline derivatives--a recent development.
TL;DR: The present review provides an insight view to pyrazolines synthesis and its biological activities along with the compilation of recent patents on pyrazoline derivatives.
Journal ArticleDOI
Synthesis and antimicrobial studies on novel chloro-fluorine containing hydroxy pyrazolines.
TL;DR: A series of chloro-fluorine containing chalcones prepared by Claisen-Schmidt condensation and tested for their antibacterial and antifungal activities, some compounds showed very good antibacterial activity and antIFungal activity.
Journal ArticleDOI
Synthesis and antimalarial evaluation of 1, 3, 5-trisubstituted pyrazolines.
B. N. Acharya,Deepika Saraswat,Mugdha Tiwari,Asish Kumar Shrivastava,Ramarao Ghorpade,Saroj Bapna,Mahabir Parshad Kaushik +6 more
TL;DR: 1,3,5-trisubstituted pyrazolines synthesized and evaluated for in vitro antimalarial efficacy against chloroquine sensitive and resistant strains of Plasmodium falciparum suggest that antimalaria mode of action of this class of compounds appears to be similar to that ofchloroquine and involves the inhibition of hemozoin formation.
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Total synthesis of natural products containing benzofuran rings
TL;DR: This review aims to highlight the origins, structures, biological potencies, and synthetic approaches of those natural products bearing at least one benzofuran in their complex structures and especially focus on the step in which this key heterocycle is installed during the total synthesis of a natural product as the desired target.
References
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Biochemistry of multidrug resistance mediated by the multidrug transporter.
Michael M. Gottesman,Ira Pastan +1 more
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Fitting curves to data using nonlinear regression: a practical and nonmathematical review.
TL;DR: This article reviews the use of nonlinear regression in a practical and nonmathematical manner to demystify non linear regression so that both its power and its limitations will be appreciated.
Journal Article
Pharmacology of drugs that alter multidrug resistance in cancer.
James M. Ford,William N. Hait +1 more
Journal Article
Bioactivities of chalcones.
TL;DR: In this article, the authors outline the different bioactivities of a variety of chalcones and describe the cytotoxic, anticancer, chemopreventative and mutagenic properties of a number of CHs followed by an account of various CHs as antimicrobial agents.
Journal Article
Rhodamine efflux patterns predict p-glycoprotein substrates in the national cancer institute drug screen
J S Lee,Kenneth D. Paull,Manuel Alvarez,Curtis Hose,Anne Monks,Michael R. Grever,A T Fojo,Susan E. Bates +7 more
TL;DR: Using the rhodamine efflux data as a seed for COMPARE analysis with the cytotoxicity data on > 30,000 compounds in the National Cancer Institute drug screen database, hundreds of compounds with high correlation coefficients were identified.