Design, synthesis and biological evaluation of potent thiazolidinedione salicylic acid inhibitors against glyoxalase-I as potential anticancer agents (Record no. 55698)
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| fixed length control field | 01916nam a2200253Ia 4500 |
| 003 - CONTROL NUMBER IDENTIFIER | |
| control field | MX-MdCICY |
| 005 - DATE AND TIME OF LATEST TRANSACTION | |
| control field | 20250626083336.0 |
| 040 ## - CATALOGING SOURCE | |
| Transcribing agency | CICY |
| 090 ## - LOCALLY ASSIGNED LC-TYPE CALL NUMBER (OCLC); LOCAL CALL NUMBER (RLIN) | |
| Classification number (OCLC) (R) ; Classification number, CALL (RLIN) (NR) | B-21631 |
| 008 - FIXED-LENGTH DATA ELEMENTS--GENERAL INFORMATION | |
| fixed length control field | 250602s9999 xx |||||s2 |||| ||und|d |
| 245 10 - TITLE STATEMENT | |
| Title | Design, synthesis and biological evaluation of potent thiazolidinedione salicylic acid inhibitors against glyoxalase-I as potential anticancer agents |
| 490 0# - SERIES STATEMENT | |
| Series statement | Medicinal Chemistry Research (2024) 33:1526-1540 |
| 500 ## - GENERAL NOTE | |
| General note | Artículo |
| 520 3# - SUMMARY, ETC. | |
| Summary, etc. | The worldwide rise in cancer incidence and mortality rates has spurred the search for new pathways implicated in cancer development and progression. One such target is glyoxalase 1 (GLO-I), a key player in methylglyoxal detoxification and a factor in the proliferation and prognosis of numerous cancers. Recent studies led by Al-Shar'i et al. utilized computer-aided drug design to identify potential inhibitors of GLO-I. The second most potent hit, (Z)-5-(5-((2,4-dioxothiazolidin-5-ylidene) methyl)furan-2-yl)-2-hydroxybenzoic acid, (IC50 = 4.24 µM), was selected as a lead for further optimization. Through molecular docking, 27 analogs were designed and evaluated for binding affinity, with 14 of the top-scorings synthesized and tested for their inhibitory activity against GLO-I. The majority of these analogs showed enhanced activities relative to the lead compound, with the most potent having an IC50 of 150 nM. These findings pave the way for the continued development of highly effective GLO-I inhibitors. |
| 650 14 - SUBJECT ADDED ENTRY--TOPICAL TERM | |
| Topical term or geographic name entry element | GLO-I ENZYME |
| 650 14 - SUBJECT ADDED ENTRY--TOPICAL TERM | |
| Topical term or geographic name entry element | MOLECULAR DOCKING |
| 650 14 - SUBJECT ADDED ENTRY--TOPICAL TERM | |
| Topical term or geographic name entry element | ARYL SALICYLIC ACID |
| 700 12 - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Alomari, B. O. |
| 700 12 - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Fakhouri, L. I. |
| 700 12 - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Al‑Shar'i, N. A. |
| 700 12 - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Albalas, Q. |
| 856 40 - ELECTRONIC LOCATION AND ACCESS | |
| Uniform Resource Identifier | <a href="https://drive.google.com/file/d/1OcpN2jN8y3WnnVYqTZlL_Ed-DDNmNmwh/view?usp=drive_link">https://drive.google.com/file/d/1OcpN2jN8y3WnnVYqTZlL_Ed-DDNmNmwh/view?usp=drive_link</a> |
| Public note | Para ver el documento ingresa a Google con tu cuenta: @cicy.edu.mx |
| 942 ## - ADDED ENTRY ELEMENTS (KOHA) | |
| Source of classification or shelving scheme | Clasificación local |
| Koha item type | Documentos solicitados |
| Lost status | Source of classification or shelving scheme | Damaged status | Not for loan | Collection | Home library | Current library | Shelving location | Date acquired | Total checkouts | Full call number | Date last seen | Price effective from | Koha item type |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Clasificación local | Ref1 | CICY | CICY | Documento préstamo interbibliotecario | 26.06.2025 | B-21631 | 26.06.2025 | 26.06.2025 | Documentos solicitados |