Abstract
Pyrazolines are five-membered heterocycles possessing two adjacent nitrogens. They have attracted significant attention from organic and medicinal chemists due to their potent biological activities and the numerous possibilities for structural diversification. In the last decade, they have been intensively studied as targets for potential anticancer therapeutics, producing a steady yearly rise in the number of published research articles. Many pyrazoline derivatives have shown remarkable cytotoxic activities in the form of heterocyclic or non-heterocyclic based hybrids, such as with coumarins, triazoles, and steroids. The enormous amount of related literature in the last 5 years prompted us to collect all these published data from screening against cancer cell lines, or protein targets like EGFR and structure activity relationship studies. Therefore, in the present review, a comprehensive account of the compounds containing the pyrazoline nucleus will be provided. The chemical groups and the structural modifications responsible for the activity will be highlighted. Moreover, emphasis will be given on recent examples from the literature and on the work of research groups that have played a key role in the development of this field.
Highlights
Pyrazolines are five-membered heterocycles possessing two adjacent nitrogens
It has been noticed that only one review exists on the therapeutic potential of steroidal pyrazolines [13], Ibnut.tJ.tMheolr.eScair. e20n20o,n2e1, r5e5g07arding the pyrazoline-hybrids in total and/or their anticancer activities. 2 of 41
Gordaliza group has reported the cytotoxic activities of many podophyllotoxin conjugates including oximes, imines, isoxazolines, pyrazoles, and pyrazolines [49]
Summary
The literature study was carried out up to April 2020 using reliable and well-established databases, namely Scopus, Google Scholar, and Reaxys. 6 and other tested analogues (Figure 6) showed unique sensitivity against MCF-7/Adr (Adriamycin-resistant cell line) over MCF-7 (for compound 6, 2.5-fold higher potency and for compound 7, 20-fold), indicating that these derivatives have potential to be developed as therapeutic agents to treat drug-resistant breast cancer. Gordaliza group has reported the cytotoxic activities of many podophyllotoxin conjugates including oximes, imines, isoxazolines, pyrazoles, and pyrazolines [49]. Among these cytotoxic fused pyrazolignans, pyrazoline 8 (N-phenyl derivative) displayed the lowest IC50 values ranging from 1.0 to 1.9 μM for P-388, A-549, and HT-29 cell lines [50,51]. Quinoline, and Other Benzene-Fused Six-Membered Heterocyclic Pyrazoline Hybrids
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
