DESIGN, SYNTHESIS AND EVALUATION OF SUBSTITUTED ARYL-2-NITROVINYL DERIVATIVES AS SMALL MOLECULES PROTEASOME INHIBITORS

Q: How can I download an article?

To download an article from SID, first log in to the site, search for the article title, and click on the 'Download Article' option.

Q: How can I download an ISI article?

To download an ISI article on SID, enter the keyword or article title in the search bar, view the relevant results, click on the desired article, and select the 'Download Article' option.

Q: How can I access the SID database?

To access the SID database, visit SID.ir, create an account, and log in to access scientific resources.

Q: Is downloading articles from SID free?

Some articles on SID are available for free, while others require payment. Details are specified on the article's page.

FAGHIH AKHLAGHI MASOUD; DAEIHAMED MARJAN; AYATOLLAHI SEYED ABDOL MAJID; KOBARFARD FARZAD; ATA ATHAR

مرکز اطلاعات علمی Scientific Information Database (SID) - Trusted Source for Research and Academic Resources

Journal Paper

Paper Information

Journal: Iranian Journal of Pharmaceutical Research Year:2018 | Volume:17 | Issue:3 Page(s): 906-916

Download Full-Text

View:

251

Download:

168

Cites:

Information Journal Paper

Title

DESIGN, SYNTHESIS AND EVALUATION OF SUBSTITUTED ARYL-2-NITROVINYL DERIVATIVES AS SMALL MOLECULES PROTEASOME INHIBITORS

Author(s)

Keywords

PROTEASOME INHIBITOR

SMALL MOLECULE

α, β-UNSATURATED NITRO

MICHAEL ACCEPTOR

ARYL-2-NITROVINYL

Abstract

Based on the existing structure activity relationship for PROTEASOME INHIBITORs, a number of substituted ARYL-2-NITROVINYL derivatives have been synthesized as MICHAEL ACCEPTOR and their cytotoxicity and PROTEASOME INHIBITORy effects were evaluated on two cancer cell lines. Compound 2d exhibited IC50 values of 0.71 and 17.79 mM comparable to bortezomib against MCF-7 and PC-3, respectively. The results show that the electronic properties and steric hindrance can affect the interaction of these SMALL MOLECULEs with their receptor at the active site of the enzyme while the presence of CH2OH group on a-carbon of MICHAEL ACCEPTOR is favorable, and para substitution of OMe on phenyl ring of b-carbon can increase the inhibitory potencies. Molecular docking studies confirm our experimental findings about mode of binding of our compounds with 20S proteasome.

Cites

No record.

References

No record.

Cite

APA: Copy

FAGHIH AKHLAGHI, MASOUD, DAEIHAMED, MARJAN, AYATOLLAHI, SEYED ABDOL MAJID, KOBARFARD, FARZAD, & ATA, ATHAR. (2018). DESIGN, SYNTHESIS AND EVALUATION OF SUBSTITUTED ARYL-2-NITROVINYL DERIVATIVES AS SMALL MOLECULES PROTEASOME INHIBITORS. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), 17(3), 906-916. SID. https://sid.ir/paper/288771/en

Vancouver: Copy

FAGHIH AKHLAGHI MASOUD, DAEIHAMED MARJAN, AYATOLLAHI SEYED ABDOL MAJID, KOBARFARD FARZAD, ATA ATHAR. DESIGN, SYNTHESIS AND EVALUATION OF SUBSTITUTED ARYL-2-NITROVINYL DERIVATIVES AS SMALL MOLECULES PROTEASOME INHIBITORS. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR)[Internet]. 2018;17(3):906-916. Available from: https://sid.ir/paper/288771/en

IEEE: Copy

MASOUD FAGHIH AKHLAGHI, MARJAN DAEIHAMED, SEYED ABDOL MAJID AYATOLLAHI, FARZAD KOBARFARD, and ATHAR ATA, “DESIGN, SYNTHESIS AND EVALUATION OF SUBSTITUTED ARYL-2-NITROVINYL DERIVATIVES AS SMALL MOLECULES PROTEASOME INHIBITORS,” IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), vol. 17, no. 3, pp. 906–916, 2018, [Online]. Available: https://sid.ir/paper/288771/en

Related Journal Papers

No record.

Related Seminar Papers

No record.

Related Plans

No record.

Recommended Workshops